Substituted pyrimidine compound and uses thereof

ABSTRACT

Disclosed is a substituted pyrimidine compound having a structure as represented by formula PY. 
     
       
         
         
             
             
         
       
     
     See the description for the definition of each substituent in the formula. The compound of the present invention provides broad-spectrum bactericidal, pesticidal, and acaricidal activities, provides great control effects against plant diseases such as cucumber downy mildew, corn rust, wheat powdery mildew, rice blast, and cucumber gray mold, specifically provides improved control effects against cucumber downy mildew, corn rust, wheat powdery mildew, and rice blast, provides great control effects against aphid, carmine spider mite, diamondback moth, and armyworm, and acquires great effects at a minimal dosage. The compound of the present invention also provides characteristics such as a simplified preparation method.

FIELD OF THE INVENTION

The invention relates to fungicide, pesticide, and acaricide.Specifically to a novel substituted pyrimidine compounds and usesthereof.

BACKGROUND OF THE INVENTION

Compounds represented by following general formula and specific compound(No. 47 compound in Patent EP0370704 and No. A compound in PatentJP2009161472) were reported in Patent EP0370704 and JP2009161472, somecompounds have some fungicidal and insecticidal activities. Known as adeveloped commercial fungicide, its English general name isdiflumetorim, and Chinese name is Fumijunan. Specific compound (No. 5compound in the literature) was also reported effective to wheat rustand barley powdery mildew in Pesticide Science. 1999 55: 896-902.

The preparation method of specific compound (No. 7 compound in PatentJP11012253) were reported in Patent JP11012253, JP11049759 andEP0665225, and its English general name is flufenerim, and Chinese nameis Michongan.

The preparation method of specific pyrimidinamine compounds representedby following general formula CK1, CK2, CK3 and CK4 (No. 83, 87, 101 and41 compounds in Patent EP0665225) were reported in Patent EP0665225,JP10036355 and U.S. Pat. No. 5,498,612, their fungicidal, insecticidaland acricidal activities were also reported.

Compounds represented by following general formula and specific compound(No. 447 compound) were reported in U.S. Pat. No. 5,925,644, somecompounds have some fungicidal, acricidal and nematicidal activities.

Disclosed in Patent EP264217, DE3786390, U.S. Pat. No. 4,895,849, U.S.Pat. No. 4,985,426 and JP63225364 are substituted pyrimidine benzylaminecompounds having a structure as represented by following formula and thespecific compound CK6 and CK7 (No. 77 and 74 compounds in PatentEP264217) applied as fungicide, insecticide and acricide.

Disclosed in Patent WO9507278 is the compound having a structure asrepresented by following formula with application as fungicide, acricideand/or insecticide. Thereinto, the specific compound CK8, CK9 and CK10were listed in No. 209 line of Table 1 without any biological activityreported.

Disclosed in U.S. Pat. No. 5,227,387 are the compound having a structureas represented by following formula and the specific compound CK11 (No.81 compound in the patent) applied as nematicide.

Compound represented by following formula and the specific compound CK12(No. 29 compound in the patent) with application as fungicide andinsecticide were disclosed in U.S. Pat. No. 5,326,766.

Compound represented by following formula and the specific compound CK13(No. 98 compound in the patent), CK14 (No. 271 compound in the patent)and CK15 (No. 117 compound in the patent) with application as fungicideand insecticide were disclosed in Patent EP534341.

Compound represented by following general formula and the specificcompound CK16 (No. 26 compound in the patent) applied as fungicide,insecticide and acricide were disclosed in Patent WO9728133.

Compound represented by following general formula and the specificcompound CK17 (No. 2.50 compound in U.S. Pat. No. 5,468,751) withapplication as fungicide, insecticide and acricide were disclosed inU.S. Pat. No. 5,468,751 and EP470600.

Compound represented by following general formula with application asinhibitor to treat HIV-1 was disclosed in Literature Bioorganic &Medicinal Chemistry Letters, 2007, 17: 260-265.

The following compound CK18 (No. 46 compound in the patent) and CK19(No. 49 compound in the patent) were reported with good insectcidalactivity at the concentration of 50 ppm and good fungicidal activity atthe concentration of 400 and 100 ppm.

The following compound CK20 (CAS No. 203734-18-3) and CK21 (CAS No.203734-22-9) were retrieved via Scifinder database without both specificliterature and biological activity disclosed.

However, substituted pyrimidine compounds represented by general formulaPY of the present invention have not been reported in prior literature.

SUMMARY OF THE INVENTION

The object of the present invention is to provide a novel substitutedpyrimidine compounds, which can be used to prepare fungicides,pesticides, and acaricides against harmful fungus, bacteria, insects,and mites in agricultural or other fields.

Detailed descriptions of the invention are as follows:

The present invention provides a kind of substituted pyrimidinecompounds having a structure as represented by general formula PY:

Wherein:

R₁ is selected from H, halo, cyano, C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl,haloC₁-C₁₂alkyl, cyanoC₁-C₁₂alkyl, cyanoC₁-C₁₂alkoxy, C₂-C₁₂alkenyl,haloC₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkynyl,C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl;

R₂ is selected from H, halo, cyano, C₃-C₁₂cycloalkyl, C₁-C₁₂alkyl,C₁-C₁₂alkoxy or haloC₁-C₁₂alkoxy;

R₃, R₄ may be the same or different, selected respectively from H, halo,OH, amino, C₁-C₁₂alkyl, C₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl,C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl, haloC₂-C₁₂alkynyl,C₁-C₁₂alkoxyC₁-C₁₂alkyl, unsubstituted or further substitutedarylC₁-C₆alkyl or heteroarylC₁-C₆alkyl by 1 to 5 following groups: halo,C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy or haloC₁-C₆alkoxy; or R₃, R₄and conjoint carbon can also form a C₃-C₈ cycle;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, OH, NO₂, cyano, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₃-C₁₂cycloalkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₂-C₁₂alkenyl, haloC₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkynyl, C₃-C₁₂alkenoxy, haloC₃-C₁₂alkenoxy, C₃-C₁₂alkynoxy,haloC₃-C₁₂alkynoxy, C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl,C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkylcarbonyloxy,C₁-C₁₂alkylcarbonylamino, C₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkoxycarbonylamino,C₁-C₁₂alkoxyC₁-C₁₂alkoxy or C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy;

X₁ is selected from N or CR₆; X₂ is selected from N or CR₇; X₃ isselected from N or CR₈;

X₄ is selected from N or CR₉; X₅ is selected from N or CR₁₀; X₆ isselected from N or CR₁₁; however, X₂, X₃, X₄, X₅, X₆ are notsimultaneously selected from N;

R₆, R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selectedrespectively from H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl,C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy,C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, halodi(C₁-C₁₂alkyl)amino, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,di(C₁-C₁₂alkyl)amino(C₁-C₁₂alkyl), CONH₂, CONHNH₂, CON(C₁-C₁₂alkyl)NH₂,CONHNH(C₁-C₁₂alkyl), CONHN(di(C₁-C₁₂alkyl)), CONHNHCO(C₁-C₁₂alkyl),CONHNHCO₂(C₁-C₁₂alkyl), CONHNH(phenyl), C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, halodi(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkylsulfonyl(C₁-C₁₂alkyl)amino,haloC₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkoxyamino,C₁-C₁₂alkoxycarbonylamino, C₁-C₁₂alkoxyaminocarbonyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁₋C₁₂alkylaminocarbonylC₁-C₁₂alkyl,di(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl,C₁₋C₁₂alkylthiocarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl, C₁₋C₁₂alkylcarbonyloxy,haloC₁-C₁₂alkylcarbonyloxy, C₁-C₁₂alkoxycarbonyloxy,haloC₁-C₁₂alkoxycarbonyloxy, C₁-C₁₂alkylaminocarbonyloxy,haloC₁-C₁₂alkylaminocarbonyloxy, C₁-C₁₂alkylsulfonyloxy,haloC₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxyC₁-C₁₂alkoxy,haloC₁-C₁₂alkoxyC₁-C₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy orhaloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy;

W is selected from H, halo, C₁-C₂alkyl, C₁-C₂alkoxy, C₁-C₂alkylthio orC₁-C₁₂alkylsulfonyl;

A is selected from O, S or NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylaminosulfonyl,di(C₁-C₁₂alkyl)aminosulfonyl, C₁-C₁₂alkylsulfonylaminocarbonyl,C₁-C₁₂alkylcarbonylaminosulfonyl, C₃-C₁₂cycloalkyloxycarbonyl,C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl,haloC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, C₂-C₁₂alkenoxycarbonyl,C₂-C₁₂alkynoxycarbonyl, C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylaminothio, di (C₁-C₁₂alkyl) aminothio, unsubstituted orfurther substituted (hetero)arylcarbonylC₁-C₆alkyl,(hetero)arylcarbonyl, (hetero)aryloxycarbonyl,(hetero)arylC₁-C₆alkyloxycarbonyl or (hetero)arylC₁-C₆alkyl by 1 to 5following groups: halo, NO₂, cyano, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy or haloC₁-C₆alkoxy;

Or the salts or complexes formed from the compounds represented bygeneral formula PY.

The technical scheme of the present invention can be further subdividedinto three optimization of technical schemes.

The first optimization of technical schemes is: the compoundsrepresented by formula PY, wherein, X₁ is selected from CR₆, X₂ isselected from N or CR₇, X₃ is selected from N or CR₈, X₄ is selectedfrom CR₉, X₅ is selected from CR₁₀, X₆ is selected from N or CR₁₁,within X₂, X₃ and X₆, at least one of which is selected from N, othersubstituents are defined as above, the compound having a structure asrepresented by formula I is as fellows.

The second optimization of technical schemes is: the compoundsrepresented by formula PY, wherein, X₁ is selected from CR₆, X₂ isselected from CR₇, X₃ is selected from CR₈, X₄ is selected from CR₉, X₅is selected from CR₁₀, X₆ is selected from CR₁₁, other substituents aredefined as above, the compound having a structure as represented byformula II is as fellows.

The third optimization of technical schemes is: the compoundsrepresented by formula PY, wherein, X₁ is selected from N, X₂ isselected from N or CR₇, X₃ is selected from N or CR₈, X₄ is selectedfrom N or CR₉, X₅ is selected from CR₁₀, X₆ is selected from N or CR₁₁,within X₂, X₃, X₄ and X₆, at least one of which is selected from N,other substituents are defined as above, the compound having a structureas represented by formula III is as fellows.

Detailed descriptions of three technical schemes of present inventionare respectively disclosed.

The first optimization of technical schemes is:

the compounds having a structure as represented by formula I are asfellows.

Wherein:

R₁ is selected from cyano, C₃-C₁₂cycloalkyl, C₁-C₁₂alkyl, halomethyl,cyanoC₁-C₂alkyl, cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl;

R₂ is selected from halo, cyano, C₃-C₁₂cycloalkyl, C₁-C₁₂alkyl orC₁-C₁₂alkoxy;

R₃, R₄ may be the same or different, selected respectively from H, halo,OH, amino, C₁-C₁₂alkyl or C₁-C₁₂alkoxy;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, OH, C₁-C₁₂alkyl or C₁-C₁₂alkoxy;

X₂ is selected from N or CR₇, X₃ is selected from N or CR₈, X₆ isselected from N or CR₁₁, within X₂, X₃, X₆, at least one substituent isselected from N;

R₉ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₁₂alkyl, haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy,C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy,haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, C₁-C₁₂alkoxycarbonyl,di(C₁-C₁₂alkyl)amino(C₁-C₁₂alkyl), haloC₁-C₁₂alkoxycarbonyl, CONH₂,CONHNH₂, CON(C₁-C₁₂alkyl)NH₂, CONHNH(C₁-C₁₂alkyl),CONHN(di(C₁-C₁₂alkyl)), CONHNHCO(C₁-C₁₂alkyl), CONHNHCO₂(C₁-C₁₂alkyl),CONHNH(phenyl), C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkylsulfonyl(C₁-C₁₂alkyl)amino,haloC₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkoxyamino,C₁-C₁₂alkoxycarbonylamino, C₁-C₁₂alkoxyaminocarbonyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl;

R₆, R₇, R₈, R₁₀, R₁₁ may be the same or different, selected respectivelyfrom H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl,C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy,C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino, di(C₁-C₁₂alkyl)amino,C₁-C₁₂alkoxycarbonyl, CONH₂, C₁-C₁₂alkylaminocarbonyl ordi(C₁-C₁₂alkyl)aminocarbonyl;

W is selected from H or C₁-C₁₂alkyl;

A is selected from O, S or NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylaminosulfonyl,di(C₁-C₁₂alkyl)aminosulfonyl, C₁-C₁₂alkylsulfonylaminocarbonyl,C₁-C₁₂alkylcarbonylaminosulfonyl, C₃-C₁₂cycloalkyloxycarbonyl,C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl,haloC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, C₂-C₁₂alkenoxycarbonyl,C₂-C₁₂alkynoxycarbonyl, C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylaminothio, di(C₁-C₁₂alkyl)aminothio, unsubstituted or furthersubstituted (hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, (hetero)arylC₁-C₆alkyloxycarbonyl or(hetero)arylC₁-C₆alkyl by 1 to 5 following groups: halo, NO₂, cyano,C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy or haloC₁-C₆alkoxy;

Or the salts or complexes formed from the compounds represented bygeneral formula I.

The preferred compounds represented by general formula I of thisinvention are:

R₁ is selected from cyano, C₃-C₆cycloalkyl, C₁-C₆alkyl, halomethyl,cyanoC₁-C₆alkyl, cyanoC₁-C₆alkoxy, C₁-C₆alkoxycarbonylC₁-C₆alkyl,C₁-C₆alkylaminocarbonylC₁-C₆alkyl ordi(C₁-C₆alkyl)aminocarbonylC₁-C₆alkyl;

R₂ is selected from halo, cyano, C₃-C₆cycloalkyl,C₁-C₆alkylorC₁-C₆alkoxy;

R₃, R₄ may be the same or different, selected respectively from H, halo,OH, amino, C₁-C₆alkyl or C₁-C₆alkoxy;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, OH, C₁-C₆alkyl or C₁-C₆alkoxy;

X₂ is selected from N or CR₇, X₃ is selected from N or CR₈, X₆ isselected from N or CR₁₁, within X₂, X₃, X₆, at least one substituent isselected from N;

R₇ is selected from H, halo, cyano or C₁-C₆alkyl;

R₆, R₈ may be the same or different, selected respectively from H, halo,cyano, C₁-C₆alkyl or C₁-C₆alkoxy;

R₉ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₆alkyl,haloC₁-C₆alkyl, C₁-C₆alkoxy, haloC₁-C₆alkoxy, C₃-C₆cycloalkyl,C₂-C₆alkenyl, C₂-C₆alkynyl, C₂-C₆alkenoxy, haloC₂-C₆alkenoxy,C₂-C₆alkynoxy, haloC₂-C₆alkynoxy, C₁-C₆alkylthio, haloC₁-C₆alkylthio,C₁-C₆alkoxyC₁-C₆alkyl, haloC₁-C₆alkoxyC₁-C₆alkyl,C₁-C₆alkylthioC₁-C₆alkyl, haloC₁-C₆alkylthioC₁-C₆alkyl,C₁-C₆alkylsulfinyl, haloC₁-C₆alkylsulfinyl, C₁-C₆alkylsulfonyl,haloC₁-C₆alkylsulfonyl, C₁-C₆alkylaminosulfonyl, C₁-C₆alkylamino,haloC₁-C₆alkylamino, di(C₁-C₆alkyl)amino, C₁-C₆alkoxycarbonyl, CONH₂,C₁-C₆alkylaminocarbonyl, di(C₁-C₆alkyl)aminocarbonyl, cyanoC₁-C₆alkoxy,C₁-C₆alkoxycarbonylC₁-C₆alkyl, C₁-C₆alkylaminocarbonylC₁-C₆alkyl ordi(C₁-C₆alkyl)aminocarbonylC₁-C₆alkyl;

R₁₀ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy, haloC₁-C₆alkoxy,C₃-C₆cycloalkyl, C₂-C₆alkenyl, C₂-C₆alkynyl, C₂-C₆alkenoxy,haloC₂-C₆alkenoxy, C₂-C₆alkynoxy, haloC₂-C₆alkynoxy, C₁-C₆alkylthio,haloC₁-C₆alkylthio, C₁-C₆alkoxyC₁-C₆alkyl, haloC₁-C₆alkoxyC₁-C₆alkyl,C₁-C₆alkylthioC₁-C₆alkyl, haloC₁-C₆alkylthioC₁-C₆alkyl,C₁-C₆alkylsulfinyl, haloC₁-C₆alkylsulfinyl, C₁-C₆alkylsulfonyl,haloC₁-C₆alkylsulfonyl, C₁-C₆alkylamino, haloC₁-C₆alkylamino,di(C₁-C₆alkyl)amino, C₁-C₆alkoxycarbonyl, CONH₂, C₁-C₆alkylaminocarbonylor di(C₁-C₆alkyl)aminocarbonyl;

R₁₁ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy, haloC₁-C₆alkoxy,C₁-C₆alkoxycarbonyl, CONH₂, C₁-C₆alkylaminocarbonyl ordi(C₁-C₆alkyl)aminocarbonyl;

W is selected from H or C₁-C₆alkyl;

A is selected from O, S or NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₆alkyl, C₁-C₆alkylcarbonyl orC₁-C₆alkylsulfonyl;

Or the salts formed from the compounds represented by general formula Iwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,formic acid, acetic acid, trifluoroacetic acid, oxalic acid,methylsulfonic acid, p-toluenesulfonic acid, benzoic acid, alizaricacid, maleic acid, sorbic acid, malic acid or citric acid.

In the general formula I, the preferred compounds represented by generalformula I-A, I-B, I-C, I-D, I-E, I-F, I-G or I-H of this invention are:

Wherein:

R₁ is selected from cyano, C₁-C₄alkyl or halomethyl;

R₂ is selected from halo, cyano, C₃-C₄cycloalkyl, C₁-C₄alkyl orC₁-C₄alkoxy;

R₃, R₄ may be the same or different, selected respectively from H, halo,OH, amino, C₁-C₄alkyl or C₁-C₄alkoxy;

R_(5b) is selected from H, halo, OH, C₁-C₄alkyl or C₁-C₄alkoxy;

R₇ is selected from H, halo, cyano or C₁-C₄alkyl;

R₈ is selected from H, halo, cyano, C₁-C₄alkyl or C₁-C₄alkoxy;

R₉ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₄alkyl,haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkylthio,haloC₁-C₄alkylthio, C₁-C₄alkoxyC₁-C₄alkyl, haloC₁-C₄alkoxyC₁-C₄alkyl,C₁-C₄alkylthioC₁-C₄alkyl, haloC₁-C₄alkylthioC₁-C₄alkyl,C₁-C₄alkylsulfinyl, haloC₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl,haloC₁-C₄alkylsulfonyl, C₁-C₄alkylaminosulfonyl, C₁-C₄alkylamino,haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino, C₁-C₄alkoxycarbonyl, CONH₂,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl, cyanoC₁-C₄alkoxy,C₁-C₄alkoxycarbonylC₁-C₄alkyl, C₁-C₄alkylaminocarbonylC₁-C₄alkyl ordi(C₁-C₄alkyl)aminocarbonylC₁-C₄alkyl;

R₁₀ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₃-C₄cycloalkyl, C₂-C₄alkenyl, C₂-C₄alkynyl, C₂-C₄alkenoxy,haloC₂-C₄alkenoxy, C₂-C₄alkynoxy, haloC₂-C₄alkynoxy, C₁-C₄alkylthio,haloC₁-C₄alkylthio, C₁-C₄alkoxyC₁-C₄alkyl, haloC₁-C₄alkoxyC₁-C₄alkyl,C₁-C₄alkylthioC₁-C₄alkyl, haloC₁-C₄alkylthioC₁-C₄alkyl,C₁-C₄alkylsulfinyl, haloC₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl,haloC₁-C₄alkylsulfonyl, C₁-C₄alkylamino, haloC₁-C₄alkylamino,di(C₁-C₄alkyl)amino, C₁-C₄alkoxycarbonyl, CONH₂, C₁-C₄alkylaminocarbonylor di(C₁-C₄alkyl)aminocarbonyl;

R₁₁ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₁-C₄alkoxycarbonyl, CONH₂, C₁-C₄alkylaminocarbonyl ordi(C₁-C₄alkyl)aminocarbonyl;

Or the salts formed from the compounds represented by general formulaI-A, I-B, I-C, I-D, I-E, I-F, I-G or I-H with hydrochloric acid,sulfuric acid, nitric acid, phosphoric acid, acetic acid,trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, benzoic acid, maleic acid, sorbic acid, malicacid or citric acid.

In the general formula I, further more, the preferred compoundsrepresented by general formula I-A, I-B, I-C, I-D, I-E, I-F, I-G or I-Hof this invention are:

R₁ is selected from cyano, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉,i-C₄H₉, t-C₄H₉, CH₂Cl, CHCl₂, CH₂F, CHF₂, CClF₂, CCl₃ or CF₃;

R₂ is selected from F, Cl, Br, cyano, CH₃, C₂H₅, OCH₃ or OC₂H₅;

R₃, R₄ may be the same or different, selected respectively from H, Cl,Br, OH, amino, CH₃, C₂H₅, OCH₃ or OC₂H₅;

R_(5b) is selected from H, Cl, Br, OH, CH₃, C₂H₅, OCH₃ or OC₂H₅;

R₇ is selected from H, Cl or cyano;

R₈ is selected from H, Cl, Br, cyano, CH₃ or OCH₃;

R₉ is selected from H, F, Cl, Br, cyano, HO(C═O), amino, NO₂, CH₃, C₂H₅,CF₃, CClF₂, OCH₃, OC₂H₅, OCF₃, COOCH₃, COOC₂H₅, CONH₂, CONHCH₃,CONHC₂H₅, CON(CH₃)₂, SO₂CH₃ or SO₂NHCH₃;

R₁₀ is selected from H, Cl, cyano, CH₃, C₂H₅, OCH₃ or OC₂H₅;

R₁₁ is selected from H, F, Cl, Br, cyano, HO(C═O), amino, NO₂, CH₃,C₂H₅, CF₃, CClF₂, OCH₃, OC₂H₅, OCF₃, COOCH₃, COOC₂H₅, CONH₂, CONHCH₃,CONHC₂H₅ or CON(CH₃)₂;

Or the salts formed from the compounds represented by general formulaI-A, I-B, I-C, I-D, I-E, I-F, I-G or I-H with hydrochloric acid,sulfuric acid, nitric acid, phosphoric acid, acetic acid,trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, maleic acid or benzoic acid.

Even more preferred compounds represented by general formula I of thisinvention are:

In the general formula I-A,

R₁ is selected from CH₃, C₂H₅, CH₂Cl, CHF₂, CClF₂, CCl₃ or CF₃;

R₂ is selected from Cl, Br or cyano;

R₃, R₄, R₁₀ is selected from H;

R_(5b) is selected from H, Cl, Br or OCH₃;

R₈ is selected from H or Cl;

R₉ is selected from H, Cl, cyano, CF₃, CClF₂, COOCH₃, COOC₂H₅ or CONH₂;

R₁ is selected from H, Cl, NO₂, CF₃, COOCH₃ or CONHCH₃;

Or, in the general formula I-B,

R₁ is selected from CH₃, C₂H₅ or CHF₂;

R₂ is selected from Cl, Br or cyano;

R₉ is selected from Cl, Br, cyano or CF₃;

R₃, R₄, R_(5b), R₁₀, R₁₁ is selected from H;

Or, in the general formula I-C,

R₁ is selected from CH₃, C₂H₅ or CHF₂;

R₂ is selected from Cl, Br or cyano;

R₃, R₄, R_(5b), R₉ is selected from H;

R₈, R₁₀ is selected from CH₃ or OCH₃;

Or, in the general formula I-E,

R₁ is selected from CH₃, C₂H₅ or CHF₂;

R₂ is selected from Cl, Br or cyano;

R₃, R₄, R_(5b), R₈, R₁₀ is selected from H;

R₉ is selected from H, Cl, cyano, CF₃, COOCH₃, COOC₂H₅ or CONH₂;

R₁ is selected from H, Cl or CF₃;

Or the salts formed from the compounds represented by general formulaI-A, I-B, I-C or I-E with hydrochloric acid, sulfuric acid, nitric acid,phosphoric acid, acetic acid, trifluoroacetic acid, oxalic acid,methylsulfonic acid, p-toluenesulfonic acid, maleic acid or benzoicacid.

Most preferred compounds represented by general formula I of thisinvention are:

In the general formula I-A,

R₁ is selected from CH₃, C₂H₅, CH₂Cl, CHF₂ or CF₃;

R₂ is selected from Cl, Br or cyano;

R₃, R₄, R_(5b), R₁₀ is selected from H;

R₉ is selected from Cl, cyano or CF₃;

R₈, R₁₁ is selected from H or Cl;

Or, in the general formula I-B,

R₁ is selected from CH₃, C₂H₅ or CHF₂;

R₂, R₉ is selected from Cl, Br or cyano;

R₃, R₄, R_(5b), R₁₀, R₁₁ is selected from H;

Or the salts formed from the compounds represented by general formulaI-A or I-B with hydrochloric acid, sulfuric acid, nitric acid,phosphoric acid, acetic acid, trifluoroacetic acid, oxalic acid,methylsulfonic acid, p-toluenesulfonic acid, maleic acid or benzoicacid.

The second optimization of technical schemes is:

The compounds having a structure as represented by formula II are asfellows.

Wherein:

R₁ is selected from C₁-C₁₂alkyl, C₃-C₈cycloalkyl or halomethyl;

R₂ is selected from halo, cyano or C₁-C₄alkoxy;

R₃, R₄ may be the same or different, selected respectively from H, halo,C₁-C₁₂alkyl, C₁-C₁₂alkoxy or C₃-C₁₂cycloalkyl; or R₃, R₄ and conjointcarbon can also form a C₃-C₈ cycle;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, OH, C₁-C₁₂alkyl or C₁-C₁₂alkoxy;

R₆, R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selectedrespectively from H, halo, OH, amino, cyano, NO₂, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂ cycloalkyl,C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino, di(C₁-C₁₂alkyl)amino,halodi(C₁-C₁₂alkyl)amino, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, halodi(C₁-C₁₂alkyl)aminocarbonyl, CONH₂,C₁-C₁₂alkylthio, haloC₁-C₁₂alkylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy,C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, haloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylcarbonyloxy,haloC₁-C₁₂alkylcarbonyloxy, C₁-C₁₂alkoxycarbonyloxy,haloC₁-C₁₂alkoxycarbonyloxy, C₁-C₁₂alkylaminocarbonyloxy,haloC₁-C₁₂alkylaminocarbonyloxy, C₁-C₁₂alkylsulfonyloxy,haloC₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxyC₁-C₁₂alkoxy,haloC₁-C₁₂alkoxyC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy orhaloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy;

W is selected from H or C₁-C₁₂alkyl;

A is selected from NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylaminosulfonyl,di(C₁-C₁₂alkyl)aminosulfonyl, C₁-C₁₂alkylsulfonylaminocarbonyl,C₁-C₁₂alkylcarbonylaminosulfonyl, C₃-C₁₂cycloalkyloxycarbonyl,C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl,haloC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, C₂-C₁₂alkenoxycarbonyl,C₂-C₁₂alkynoxycarbonyl, C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylaminothio, di (C₁-C₁₂alkyl) aminothio, unsubstituted orfurther substituted (hetero)arylcarbonylC₁-C₆alkyl,(hetero)arylcarbonyl, (hetero)aryloxycarbonyl,(hetero)arylC₁-C₆alkyloxycarbonyl or (hetero)arylC₁-C₆alkyl by 1 to 5following groups: halo, NO₂, cyano, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy or haloC₁-C₆alkoxy;

Or the salts or complexes formed from the compounds of general formulaII.

The preferred compounds represented by general formula II of thisinvention are:

R₁ is selected from C₁-C₆alkyl, C₃-C₆cycloalkyl or halomethyl;

R₂ is selected from halo, cyano or C₁-C₄alkoxy;

R₃, R₄ may be the same or different, selected respectively from H, halo,C₁-C₆alkyl, C₁-C₆alkoxy or C₃-C₆cycloalkyl; or R₃, R₄ and conjointcarbon can also form a C₃-C₈ cycle;

R_(5a), R_(5b), R_(5c), R₆ may be the same or different, selectedrespectively from H, halo, OH, C₁-C₆alkyl or C₁-C₆alkoxy;

R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selected respectivelyfrom H, halo, OH, amino, cyano, NO₂, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy, haloC₁-C₆alkoxy, C₃-C₆cycloalkyl, C₁-C₆alkylamino,haloC₁-C₆alkylamino, di(C₁-C₆alkyl)amino, halodi(C₁-C₆alkyl)amino,C₁-C₆alkylaminocarbonyl, di(C₁-C₆alkyl)aminocarbonyl,halodi(C₁-C₆alkyl)aminocarbonyl, CONH₂, C₁-C₆alkylthio,haloC₁-C₆alkylthio, C₂-C₆alkenyl, C₂-C₆alkynyl, C₂-C₆alkenoxy,haloC₂-C₆alkenoxy, C₂-C₆alkynoxy, haloC₂-C₆alkynoxy, C₁-C₆alkylsulfonyl,haloC₁-C₆alkylsulfonyl, C₁-C₆alkylcarbonyl, haloC₁-C₆alkylcarbonyl,C₁-C₆alkoxycarbonyl, haloC₁-C₆alkoxycarbonyl, C₁-C₆alkoxyC₁-C₆alkyl,haloC₁-C₆alkoxyC₁-C₆alkyl, C₁-C₆alkylthioC₁-C₆alkyl,haloC₁-C₆alkylthioC₁-C₆alkyl, C₁-C₆alkoxycarbonylC₁-C₆alkyl,haloC₁-C₆alkoxycarbonylC₁-C₆alkyl, C₁-C₆alkylthiocarbonylC₁-C₆alkyl,haloC₁-C₆alkylthiocarbonylC₁-C₆alkyl, C₁-C₆alkylcarbonyloxy,haloC₁-C₆alkylcarbonyloxy, C₁-C₆alkoxycarbonyloxy,haloC₁-C₆alkoxycarbonyloxy, C₁-C₆alkylaminocarbonyloxy,haloC₁-C₆alkylaminocarbonyloxy, C₁-C₆alkylsulfonyloxy,haloC₁-C₆alkylsulfonyloxy, C₁-C₆alkoxyC₁-C₆alkoxy,haloC₁-C₆alkoxyC₁-C₆alkoxy, C₁-C₆alkoxycarbonylC₁-C₆alkoxy orhaloC₁-C₆alkoxycarbonylC₁-C₆alkoxy;

W is selected from H or C₁-C₃alkyl;

A is selected from NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₆alkyl, C₁-C₆alkylsulfonyl orC₁-C₆alkylcarbonyl;

Or the salts formed from the compounds represented by general formula IIwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,formic acid, acetic acid, trifluoroacetic acid, oxalic acid,methylsulfonic acid, p-toluenesulfonic acid, benzoic acid, alizaricacid, maleic acid, sorbic acid, malic acid or citric acid.

Further more, the preferred compounds represented by general formula IIof this invention are:

R₁ is selected from C₁-C₄alkyl, C₃-C₄cycloalkyl or halomethyl;

R₂ is selected from F, Cl, Br or cyano;

R₃, R₄ may be the same or different, selected respectively from H, halo,C₁-C₄alkyl, C₁-C₄alkoxy or C₃-C₆cycloalkyl; or R₃, R₄ and conjointcarbon can also form a C₃-C₈ cycle;

R_(5a), R_(5b), R_(5c), R₆ may be the same or different, selectedrespectively from H, halo, OH, C₁-C₄alkyl or C₁-C₄alkoxy;

R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selected respectivelyfrom H, halo, OH, amino, cyano, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl,C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₃-C₄cycloalkyl, C₁-C₄alkylamino,haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino, halodi(C₁-C₄alkyl)amino,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl,halodi(C₁-C₄alkyl)aminocarbonyl, CONH₂, C₁-C₄alkylthio,haloC₁-C₄alkylthio, C₂-C₄alkenyl, C₂-C₄alkynyl, C₂-C₄alkenoxy,haloC₂-C₄alkenoxy, C₂-C₄alkynoxy, haloC₂-C₄alkynoxy, C₁-C₄alkylsulfonyl,haloC₁-C₄alkylsulfonyl, C₁-C₄alkylcarbonyl, haloC₁-C₄alkylcarbonyl,C₁-C₄alkoxycarbonyl, haloC₁-C₄alkoxycarbonyl, C₁-C₄alkoxyC₁-C₄alkyl,haloC₁-C₄alkoxyC₁-C₄alkyl, C₁-C₄alkylthioC₁-C₄alkyl,haloC₁-C₄alkylthioC₁-C₄alkyl, C₁-C₄alkoxycarbonylC₁-C₄alkyl,haloC₁-C₄alkoxycarbonylC₁-C₄alkyl, C₁-C₄alkylthiocarbonylC₁-C₄alkyl,haloC₁-C₄alkylthiocarbonylC₁-C₄alkyl, C₁-C₄alkylcarbonyloxy,haloC₁-C₄alkylcarbonyloxy, C₁-C₄alkoxycarbonyloxy,haloC₁-C₄alkoxycarbonyloxy, C₁-C₄alkylaminocarbonyloxy,haloC₁-C₄alkylaminocarbonyloxy, C₁-C₄alkylsulfonyloxy,haloC₁-C₄alkylsulfonyloxy, C₁-C₄alkoxyC₁-C₄alkoxy,haloC₁-C₄alkoxyC₁-C₄alkoxy, C₁-C₄alkoxycarbonylC₁-C₄alkoxy orhaloC₁-C₄alkoxycarbonylC₁-C₄alkoxy;

W is selected from H or CH₃;

A is selected from NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₄alkyl, C₁-C₄alkylsulfonyl orC₁-C₄alkylcarbonyl;

Or the salts formed from the compounds represented by general formula IIwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, benzoic acid, maleic acid, sorbic acid, malicacid or citric acid.

Even more preferred compounds represented by formula II of thisinvention are:

R₁ is selected from CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉,t-C₄H₉, cyclopropyl, cyclobutyl, CF₃, CCl₃, CH₂F, CH₂Cl, CH₂Br, CClF₂,CCl₂F, CHF₂ or CHCl₂;

R₂ is selected from F, Cl, Br or cyano;

R₃, R₄ may be the same or different, selected respectively from H, F,Cl, Br, I, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉,OCH₃, OC₂H₅, OC₃H₇-n, OC₃H₇-i, OC₄H₉-n, OC₄H₉-s, OC₄H₉-i or OC₄H₉-t;

R_(5a), R_(5b), R_(5c), R₆ may be the same or different, selectedrespectively from H, F, Cl, Br, I, OH, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇,n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, OCH₃, OC₂H₅, OC₃H₇-n, OC₃H₇-i, OC₄H₉-n,OC₄H₉-s, OC₄H₉-i or OC₄H₉-t;

R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selected respectivelyfrom H, F, Cl, Br, I, cyano, amino, NO₂, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇,n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, CF₃, CCl₃, CClF₂, CCl₂F, CHCl₂, CH₂F,CHF₂, OCH₃, OC₂H₅, OC₃H₇-n, OC₃H₇-i, OC₄H₉-n, OC₄H₉-s, OC₄H₉-i, OC₄H₉-t,OCF₃, OCH₂CF₃, COOCH₃, COOC₂H₅, CONH₂, CONHCH₃, CONHC₂H₅, CONH(CH₃)₂,methylsulfonyl or trifluoromethylsulfonyl;

W is selected from H or CH₃;

A is selected from NR₁₂;

B is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H;

Or the salts formed from the compounds represented by general formula IIwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, maleic acid or benzoic acid.

Even further more preferred compounds represented by formula II of thisinvention are:

R₁ is selected from CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉,t-C₄H₉, cyclopropyl, cyclobutyl, CH₂Cl, CHCl₂, CH₂F, CHF₂, CClF₂, CCl₃or CF₃;

R₂ is selected from F, Cl, Br or cyano;

R₃, R₄ may be the same or different, selected respectively from H, F,Cl, Br, I, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, OCH₃, OC₂H₅, OC₃H₇-n or OC₃H₇-i;

R_(5a), R_(5b), R_(5c), R₆ may be the same or different, selectedrespectively from H, F, Cl, Br or OCH₃;

R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selected respectivelyfrom H, F, Cl, Br, I, cyano, NO₂, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉,s-C₄H₉, i-C₄H₉, t-C₄H₉, OCH₃, OCF₃, CF₃, CCl₃, CClF₂, CCl₂F, CHCl₂,CH₂F, CHF₂, methylsulfonyl or trifluoromethylsulfonyl;

W is selected from H or CH₃;

A is selected from NH;

B is selected from —CH₂— or —CH₂CH₂—;

Or the salts formed from the compounds of general formula II withhydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, aceticacid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, maleic acid or benzoic acid.

Most preferred compounds represented by formula II of this inventionare:

R₁ is selected from CH₃, C₂H₅, CHF₂ or CF₃;

R₂ is selected from Cl or cyano;

R₃, R₄ is selected from H;

R_(5a), R_(5b), R_(5c), R₆ may be the same or different, selectedrespectively from H, F, Cl, Br or OCH₃;

W is selected from H or CH₃;

R₇, R₈, R₉, R₁₀, R₁₁ may be the same or different, selected respectivelyfrom H, F, Cl, cyano, NO₂, CH₃, OCH₃, OCF₃, CF₃ or methylsulfonyl;

A is selected from NH;

B is selected from —CH₂— or —CH₂CH₂—;

Or the salts formed from the compounds represented by general formula IIwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,acetic acid or trifluoroacetic acid.

The third optimization of technical schemes is:

the compounds having a structure as represented by formula III are asfellows.

R₁ is selected from halo, C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl,haloC₁-C₁₂alkyl, C₂-C₁₂alkenyl, haloC₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl orhaloC₁-C₁₂alkoxyC₁-C₁₂alkyl;

R₂ is selected from halo, cyano, C₁-C₁₂alkyl, C₁-C₁₂alkoxy orhaloC₁-C₁₂alkoxy;

W is selected from H, halo, C₁-C₁₂alkyl, C₁-C₁₂alkoxy, C₁-C₁₂alkylthioor C₁-C₁₂alkylsulfonyl;

R₃, R₄ may be the same or different, selected respectively from H,C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkenyl, haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl,unsubstituted or further substituted arylC₁-C₆alkyl orheteroarylC₁-C₆alkyl by 1 to 5 following groups: halo, C₁-C₆alkyl,haloC₁-C₆alkyl, C₁-C₆alkoxy or haloC₁-C₆alkoxy; or R₃, R₄ and conjointcarbon can also form a C₃-C₈ cycle;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, NO₂, cyano, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₃-C₁₂cycloalkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₂-C₁₂alkenyl, haloC₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkynyl, C₃-C₁₂alkenoxy, haloC₃-C₁₂alkenoxy, C₃-C₁₂alkynoxy,haloC₃-C₁₂alkynoxy, C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl,C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkylcarbonyloxy,C₁-C₁₂alkylcarbonylamino, C₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkoxycarbonylamino,C₁-C₁₂alkoxyC₁-C₁₂alkoxy or C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy;

X₂ is selected from N or CR₇;

X₃ is selected from N or CR₈;

X₄ is selected from N or CR₉;

X₆ is selected from N or CR₁₁; however, X₂, X₃, X₄, X₆ are notsimultaneously selected from N;

R₇, R₈, R₉, R₁ may be the same or different, selected respectively fromH, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonyl, CONH₂,C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonyl or haloC₁-C₁₂alkylsulfonyl;

R₁₀ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₁₂alkyl, haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy,C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy,haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, C₁-C₁₂alkoxycarbonyl, CONH₂,C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl;

A is selected from O, S or NR₁₂;

B is selected from is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylaminosulfonyl,di(C₁-C₁₂alkyl)aminosulfonyl, C₁-C₁₂alkylsulfonylaminocarbonyl,C₁-C₁₂alkylcarbonylaminosulfonyl, C₃-C₁₂cycloalkyloxycarbonyl,C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl,haloC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, C₂-C₁₂alkenoxycarbonyl,C₂-C₁₂alkynoxycarbonyl, C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylaminothio, di(C₁-C₁₂alkyl)aminothio, unsubstituted or furthersubstituted (hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, (hetero)arylC₁-C₆alkyloxycarbonyl or(hetero)arylC₁-C₆alkyl by 1 to 5 following groups: halo, NO₂, cyano,C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy or haloC₁-C₆alkoxy;

Or the salts or complexes formed from the compounds represented bygeneral formula III.

The preferred compounds represented by general formula III of thisinvention are:

R₁ is selected from halo, C₁-C₈alkyl, C₃-C₈cycloalkyl, haloC₁-C₈alkyl,C₂-C₈alkenyl, haloC₂-C₈alkenyl, C₂-C₈alkynyl, haloC₂-C₈alkynyl,C₁-C₈alkoxyC₁-C₈alkyl or haloC₁-C₈alkoxyC₁-C₈alkyl;

R₂ is selected from halo, cyano, C₁-C₈alkyl, C₁-C₈alkoxy orhaloC₁-C₈alkoxy;

W is selected from H, halo, C₁-C₈alkyl, C₁-C₈alkoxy, C₁-C₈alkylthio orC₁-C₈alkylsulfonyl;

R₃, R₄ may be the same or different, selected respectively from H,C₁-C₈alkyl, C₃-C₈cycloalkyl, C₂-C₈alkenyl, C₂-C₈alkynyl,haloC₂-C₈alkenyl, haloC₂-C₈alkynyl, C₁-C₈alkoxyC₁-C₈alkyl, unsubstitutedor further substituted arylC₁-C₄alkyl or heteroarylC₁-C₄alkyl by 1 to 3following groups: halo, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy orhaloC₁-C₄alkoxy; or R₃, R₄ and conjoint carbon can also form a C₃-C₈cycle;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, NO₂, cyano, C₁-C₈alkyl, haloC₁-C₈alkyl,C₃-C₆cycloalkyl, C₁-C₈alkoxy, haloC₁-C₈alkoxy, C₁-C₈alkylthio,haloC₁-C₈alkylthio, C₂-C₈alkenyl, haloC₂-C₈alkenyl, C₂-C₈alkynyl,haloC₂-C₈alkynyl, C₃-C₈alkenoxy, haloC₃-C₈alkenoxy, C₃-C₈alkynoxy,haloC₃-C₈alkynoxy, C₁-C₈alkylsulfinyl, haloC₁-C₈alkylsulfinyl,C₁-C₈alkylsulfonyl, haloC₁-C₈alkylsulfonyl, C₁-C₈alkylcarbonyl,haloC₁-C₈alkylcarbonyl, C₁-C₈alkylcarbonyloxy, C₁-C₈alkylcarbonylamino,C₁-C₈alkylsulfonyloxy, C₁-C₈alkoxycarbonyl,C₁-C₈alkoxycarbonylC₁-C₈alkyl, C₁-C₈alkoxycarbonylamino,C₁-C₈alkoxyC₁-C₈alkoxy or C₁-C₈alkoxycarbonylC₁-C₈alkoxy;

X₂ is selected from N or CR₇;

X₃ is selected from N or CR₈;

X₄ is selected from N or CR₉;

X₆ is selected from N or CR₁₁; however, X₂, X₃, X₄, X₆ are notsimultaneously selected from N;

R₇, R₈, R₉, R₁₁ may be the same or different, selected respectively fromH, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₈alkyl, haloC₁-C₈alkyl,C₁-C₈alkoxy, haloC₁-C₈alkoxy, C₁-C₈alkoxycarbonyl, CONH₂,C₁-C₈alkylaminocarbonyl, di(C₁-C₈alkyl)aminocarbonyl, C₁-C₈alkylsulfonylor haloC₁-C₈alkylsulfonyl;

R₁₀ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₈alkyl, haloC₁-C₈alkyl, C₁-C₈alkoxy, haloC₁-C₈alkoxy,C₃-C₈cycloalkyl, C₂-C₈alkenyl, C₂-C₈alkynyl, C₂-C₈alkenoxy,haloC₂-C₈alkenoxy, C₂-C₈alkynoxy, haloC₂-C₈alkynoxy, C₁-C₈alkylthio,haloC₁-C₈alkylthio, C₁-C₈alkoxyC₁-C₈alkyl, haloC₁-C₈alkoxyC₁-C₈alkyl,C₁-C₈alkylthioC₁-C₈alkyl, haloC₁-C₈alkylthioC₁-C₈alkyl,C₁-C₈alkylsulfinyl, haloC₁-C₈alkylsulfinyl, C₁-C₈alkylsulfonyl,haloC₁-C₈alkylsulfonyl, C₁-C₈alkylaminosulfonyl, C₁-C₈alkylamino,haloC₁-C₈alkylamino, di(C₁-C₈alkyl)amino, C₁-C₈alkoxycarbonyl, CONH₂,C₁-C₈alkylaminocarbonyl, di(C₁-C₈alkyl)aminocarbonyl, cyanoC₁-C₈alkoxy,C₁-C₈alkoxycarbonylC₁-C₈alkyl, C₁-C₈alkylaminocarbonylC₁-C₈alkyl ordi(C₁-C₈alkyl)aminocarbonylC₁-C₈alkyl;

A is selected from O, S or NR₁₂;

B is selected from is selected from —CH₂— or —CH₂CH₂—;

R₁₂ is selected from H, OH, H(C)═O, C₁-C₈alkyl, haloC₁-C₈alkyl,C₁-C₈alkoxy, haloC₁-C₈alkoxy, C₃-C₈cycloalkyl, C₁-C₈alkylthio,C₂-C₈alkenylthio, C₂-C₈alkenyl, C₂-C₈alkynyl, haloC₂-C₈alkenyl,haloC₂-C₈alkynyl, C₁-C₈alkoxyC₁-C₈alkyl, haloC₁-C₈alkoxyC₁-C₈alkyl,C₁-C₈alkylthioC₁-C₈alkyl, haloC₁-C₈alkylthioC₁-C₈alkyl,C₁-C₈alkylsulfinyl, haloC₁-C₈alkylsulfinyl, C₁-C₈alkylsulfonyl,haloC₁-C₈alkylsulfonyl, C₁-C₈alkylaminosulfonyl,di(C₁-C₈alkyl)aminosulfonyl, C₁-C₈alkylsulfonylaminocarbonyl,C₁-C₈alkylcarbonylaminosulfonyl, C₃-C₈cycloalkyloxycarbonyl,C₁-C₈alkylcarbonyl, haloC₁-C₈alkylcarbonyl, C₁-C₈alkoxycarbonyl,haloC₁-C₈alkoxycarbonyl, C₁-C₈alkylcarbonylC₁-C₈alkyl,C₁-C₈alkoxycarbonylC₁-C₈alkyl, C₁-C₈alkylaminocarbonyl,di(C₁-C₈alkyl)aminocarbonyl, C₂-C₈alkenoxycarbonyl,C₂-C₈alkynoxycarbonyl, C₁-C₈alkoxyC₁-C₈alkoxycarbonyl,C₁-C₈alkylaminothio, di (C₁-C₈alkyl) aminothio, unsubstituted or furthersubstituted (hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, (hetero)arylC₁-C₆alkyloxycarbonyl or(hetero)arylC₁-C₆alkyl by 1 to 3 following groups: halo, NO₂, cyano,C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy or haloC₁-C₄alkoxy;

Or the salts formed from the compounds represented by general formulaIII.

Further more, the preferred compounds represented by general formula IIIof this invention are:

R₁ is selected from halo, C₁-C₄alkyl, C₃-C₆cycloalkyl, haloC₁-C₄alkyl,C₂-C₄alkenyl, haloC₂-C₄alkenyl, C₂-C₄alkynyl, haloC₂-C₄alkynyl,C₁-C₄alkoxyC₁-C₄alkyl or haloC₁-C₄alkoxyC₁-C₄alkyl;

R₂ is selected from halo or cyano;

W is selected from H or CH₃;

R₃, R₄ is selected from H, CH₃ or C₂H₅;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, halo, NO₂, cyano, C₁-C₄alkyl, haloC₁-C₄alkyl,C₃-C₆cycloalkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkylthio,haloC₁-C₄alkylthio, C₂-C₄alkenyl, C₂-C₄alkynyl, C₁-C₄alkylsulfinyl,C₁-C₄alkylsulfonyl, C₁-C₄alkylcarbonyl or C₁-C₄alkoxyC₁-C₄alkoxy;

X₂ is selected from N or CR₇;

X₃ is selected from N or CR₈;

X₄ is selected from N or CR₉;

X₆ is selected from N or CR₁₁; however, X₂, X₃, X₄, X₆ are notsimultaneously selected from N;

R₇, R₈, R₉, R₁₁ may be the same or different, selected respectively fromH, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl,C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkoxycarbonyl, CONH₂,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl orC₁-C₄alkylsulfonyl or haloC₁-C₄alkylsulfonyl;

R₁₀ is selected from H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₃-C₄cycloalkyl, C₂-C₄alkenyl, C₂-C₄alkynyl, C₂-C₄alkenoxy,haloC₂-C₄alkenoxy, C₂-C₄alkynoxy, haloC₂-C₄alkynoxy, C₁-C₄alkylthio,haloC₁-C₄alkylthio, C₁-C₄alkoxyC₁-C₄alkyl, haloC₁-C₄alkoxyC₁-C₄alkyl,C₁-C₄alkylthioC₁-C₄alkyl, haloC₁-C₄alkylthioC₁-C₄alkyl,C₁-C₄alkylsulfinyl, haloC₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl,haloC₁-C₄alkylsulfonyl, C₁-C₄alkylaminosulfonyl, C₁-C₄alkylamino,haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino, C₁-C₄alkoxycarbonyl, CONH₂,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl, cyanoC₁-C₁₂alkoxy,C₁-C₄alkoxycarbonylC₁-C₄alkyl, C₁-C₄alkylaminocarbonylC₁-C₄alkyl ordi(C₁-C₄alkyl)aminocarbonylC₁-C₄alkyl;

A is selected from O, S or NH;

B is selected from —CH₂— or —CH₂CH₂—;

Or the salts formed from the compounds represented by general formulaIII with hydrochloric acid, sulfuric acid, phosphoric acid, formic acid,acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid, sorbicacid, malic acid or citric acid.

In the general formula III, even more preferred compounds represented bygeneral formula III-A, III-B, III-C, III-D, III-E, III-F, III-G, III-H,III-I or III-J of this invention are:

Wherein:

R₁ is selected from F, Cl, Br, I, C₁-C₄alkyl, C₃-C₆cycloalkyl,haloC₁-C₄alkyl, C₂-C₄alkenyl, C₂-C₄alkynyl, C₁-C₄alkoxyC₁-C₄alkyl orhaloC₁-C₄alkoxyC₁-C₄alkyl;

R₂ is selected from halo or cyano;

W is selected from H or CH₃;

R₃, R₄ is selected from H, CH₃ or C₂H₅;

R_(5a), R_(5b), R_(5c) may be the same or different, selectedrespectively from H, F, Cl, Br, I, NO₂, cyano, C₁-C₄alkyl,haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy or C₁-C₄alkylcarbonyl;

R₇, R₈, R₉, R₁₁ may be the same or different, selected respectively fromH, F, Cl, Br, I, cyano, HO(C═O), NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl,C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkoxycarbonyl,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl, C₁-C₄alkylsulfonylor haloC₁-C₄alkylsulfonyl;

R₁₀ is selected from H, F, Cl, Br, I, cyano, NO₂, C₁-C₄alkyl,haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkylsulfonyl orhaloC₁-C₄alkylsulfonyl;

A is selected from O, S or NH;

Or the salts formed from the compounds represented by general formulaIII-A, III-B, III-C, III-D, III-E, III-F, III-G, III-H, III-I or III-Jwith hydrochloric acid, sulfuric acid, phosphoric acid, formic acid,acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid, sorbicacid, malic acid or citric acid.

Even further more preferred compounds represented by formula III of thisinvention are:

R₁ is selected from Cl, CH₃, C₂H₅, CHCl₂, CCl₃, CH₂F, CClF₂, CHF₂ orCF₃;

R₂ is selected from halo or cyano;

W is selected from H or CH₃;

R₃, R₄ is selected from H;

R_(5a), R_(5c) is selected from H;

R_(5b) is selected from H, F, Cl, Br or OCH₃;

R₇, R₈, R₉, R₁₁ may be the same or different, selected respectively fromH, F, Cl, Br, cyano, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy,haloC₁-C₄alkoxy, C₁-C₄alkoxycarbonyl, C₁-C₄alkylaminocarbonyl,di(C₁-C₄alkyl)aminocarbonyl, C₁-C₄alkylsulfonyl orhaloC₁-C₄alkylsulfonyl;

R₁₀ is selected from H, F, Cl, Br, I, cyano, NO₂, methylsulfonyl,C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy or haloC₁-C₄alkoxy;

A is selected from NH;

Or the salts formed from the compounds represented by general formulaIII-A with hydrochloric acid, sulfuric acid, phosphoric acid, formicacid, acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonicacid, p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid,sorbic acid, malic acid or citric acid.

Most preferred compounds represented by formula III of this inventionare:

In the general formula III-A,

R₁ is selected from Cl, CH₃, C₂H₅, CHF₂ or CF₃;

R₂ is selected from Cl or cyano;

W is selected from H or CH₃;

R₃, R₄ is selected from H;

R_(5a), R_(5c) is selected from H;

R_(5b) is selected from H, Cl or OCH₃;

R₇, R₈, R₉, R may be the same or different, selected respectively fromH, F, Cl, CH₃, cyano, NO₂, CF₃, CClF₂, CCl₃, OCH₃, OCF₃, OCH₂CF₃,methylsulfonyl or trifluorosulfonyl;

R₁₀ is selected from H, F, Cl, CH₃, cyano, NO₂, methylsulfonyl, CF₃,CClF₂, OCH₃, OCF₃ or OCH₂CF₃;

A is selected from NH;

Or the salts formed from the compounds represented by general formulaIII-A with hydrochloric acid, sulfuric acid, phosphoric acid, formicacid, acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonicacid, p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid,sorbic acid, malic acid or citric acid.

The terms of substitutes used above to definite the compoundsrepresented by general formula PY are as follows:

The “halogen” or “halo” is fluorine, chlorine, bromine or iodine.

The “alkyl” stands for straight or branched chain alkyl, such as methyl,ethyl, propyl, isopropyl or tert-butyl.

The “cycloalkyl” is substituted or unsubstituted cyclic alkyl, such ascyclopropyl, cyclopentyl or cyclohexyl. The substitute(s) is(are)methyl, halogen, etc.

The “haloalkyl” stands for straight or branched chain alkyl, in whichhydrogen atoms can be all or partly substituted with halogen, such aschloromethyl, dichloromethyl, trichloromethyl, fluoromethyl,difluoromethyl, trifluoromethyl, etc.

The “alkoxy” refers to straight or branched chain alkyl, which is linkedto the structure by oxygen atom. The “haloalkoxy” refers to straight orbranched chain alkoxy, in which hydrogen atoms may be all or partlysubstituted with halogen, such as chloromethoxy, dichloromethoxy,trichloromethoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy,chlorofluoromethoxy, trifluoroethoxy, etc. The “alkylthio” refers tostraight or branched chain alkyl, which is linked to the structure bysulfur atom. The “haloalkylthio” refers to straight or branched chainalkylthio, in which hydrogen atoms may be all or partly substituted withhalogen, such as chloromethylthio, dichloromethylthio,trichloromethylthio, fluoromethylthio, difluoromethylthio,trifluoromethylthio, chlorofluoromethylthio, etc.The “cyanoalkyl” refers to straight or branched chain alkyl, in whichhydrogen atoms may be all or partly substituted with cyano, such as—CH₂CN, —CH₂CH₂CN, —CH₂C(CH₃)₂ CN, —CH₂CH(CN)₂, etc. The “cyanoalkoxy”refers to alkoxy, in which hydrogen atoms may be all or partlysubstituted with cyano, such as —OCH₂CN. The “haloalkylamino” refers tostraight or branched chain alkylamino, in which hydrogen atoms may beall or partly substituted with halogen. The “dialkylamino” such as—N(CH₃)₂, —N(CH₃CH₂)₂. The “dihaloalkylamino” such as —N(CF₃)₂,—N(CH₂CCl₃)₂. The “dialkylaminoalkyl” such as —CH₂N(CH₃)₂.The “alkenyl” refers to straight or branched chain alkenyl, such asethenyl, 1-propenyl, 2-propenyl and different isomer of butenyl,pentenyl and hexenyl. Alkenyl also includes polyene, such aspropa-1,2-dienyl and hexa-2,4-dienyl. The “haloalkenyl” stands forstraight or branched chain alkenyl, in which hydrogen atoms can be allor partly substituted with halogen. The “alkynyl” refers to straight orbranched chain alkynyl, such as ethynyl, 1-propynyl, 2-propynyl anddifferent isomer of butynyl, pentynyl and hexynyl. Alkynyl also includesgroups including more than one triple bonds, such as hexa-2,5-diynyl.The “haloalkynyl” stands for straight or branched chain alkynyl, inwhich hydrogen atoms can be all or partly substituted with halogen.The alkenoxyl refers to straight or branched chain alkynes is linked tothe structure by oxygen, The haloalkenoxyl stands for a straight-chainor branched alkenoxyl, in which hydrogen atoms may be all or partlysubstituted with halogen. The alkynoxyl refers to straight or branchedchain alkynes is linked to the structure by oxygen. The haloalkynoxylstands for a straight-chain or branched alkynoxyl, in which hydrogenatoms may be all or partly substituted with halogen.The “alkylsulfinyl” means a straight-chain or branched alkyl is linkedto the structure by (—SO—), such as methylsulfinyl.The “haloalkylsulfinyl” stands for a straight-chain or branchedalkylsulfinyl, in which hydrogen atoms may be all or partly substitutedwith halogen.The “alkylsulfonyl” means a straight-chain or branched alkyl is linkedto the structure by (—SO₂—), such as methylsulfonyl.The “haloalkylsulfonyl” stands for a straight-chain or branchedalkylsulfonyl, in which hydrogen atoms may be all or partly substitutedwith halogen.The “alkylcarbonyl” means alkyl is linked to the structure by carbonyl,such as —COCH₃, —COCH₂CH₃. The “haloalkylcarbonyl” stands for astraight-chain or branched alkylcarbonyl, in which hydrogen atoms may beall or partly substituted with halogen, such as —COCF₃. The“alkoxyalkyl” means alkyl-O-alkyl-, such as —CH₂OCH₃. The“haloalkoxyalkyl” refers to alkoxyalkyl, in which hydrogen atom may beall or partyl substituted with halogen, such as —CH₂OCH₂CH₂Cl. The“alkylthioalkyl” means alkyl-S-alkyl-, such as —CH₂SCH₃. The“haloalkylthioalkyl” refers to alkylthioalkyl, in which hydrogen atommay be all or partyl substituted with halogen, such as —CH₂SCH₂CH₂Cl,—CH₂SCH₂CF₃.The “alkoxycarbonyl” means alkoxy is linked to the structure bycarbonyl, such as —COOCH₃, —COOCH₂CH₃. The “haloalkoxycarbonyl” refersto straight or branched chain alkoxycarbonyl, in which hydrogen atomscan be all or partly substituted with halogen. The “alkylaminocarbonyl”means alkyl-NH—CO—, such as —CONHCH₃, —CONHCH₂CH₃. The“dialkylaminocarbonyl” such as —CON(CH₃)₂, —CON(CH₂CH₃)₂.The “halodialkylaminocarbonyl” such as —CON(CF₃)₂, —CON(CH₂CCl₃)₂.The “alkoxycarbonylalkyl” such as —CH₂COOCH₃, —CH₂COOCH₂CH₃. The“haloalkoxycarbonylalkyl” such as —CH₂COOCF₃, —CH₂COOCH₂CF₃.The “alkoxycarbonylamino” such as —NHCOOCH₃, —NHCOOCH₂CH₃. The“alkoxyaminocarbonyl” such as —CONHOCH₃, —CONHOCH₂CH₃. The“alkylaminocarbonylalkyl” such as —CH₂CONHCH₃, —CH₂CONHCH₂CH₃.“dialkylaminocarbonylalkyl” such as —CH₂CON(CH₃)₂, —CH₂CON(CH₂CH₃)₂.The “alkenylthio” refers to straight or branched chain alkenyl, which islinked to the structure by sulfur atom. Such as —SCH₂CH═CH₂. The“cycloalkyloxycarbonyl” means cyclopropyloxycarbonyl,cyclohexyloxycarbonyl, etc.The “alkenoxylcarbonyl” means CH₂═CHCH₂OCO—. The “alkynoxylcarbonyl”means —COOCH₂C≡CH. The “alkoxyamino”: such as —NHOCH₃. The“alkoxyalkoxycarbonyl”: such as —COOCH₂CH₂OCH₃, etc. The“alkylaminothio” refers to —SNHCH₃, —SNHC₂H₅. The “dialkylaminothio”refers to —SN(CH₃)₂, —SN(C₂H₅)₂.The “alkylcarbonylalkyl” refers to alkyl-CO-alkyl-. The“alkylsulfonylamino” refers to alkyl-SO₂—NH—. The“haloalkylsulfonylamino” refers to straight or branched chainalkylsulfonylamino, in which hydrogen atoms can be all or partlysubstituted with halogen.The “alkylsulfonylalkylamino” refers to alkyl-SO₂-alkyl-NH—.The “alkylaminosulfonyl” refers to alkyl-NH—SO₂—.The“alkylcarbonylaminosulfonyl” refers to alkyl-CO—NH—SO₂—. The“dialkylaminosulfonyl” refers to (alkyl)₂-N—SO₂—.The “alkylthiocarbonylalkyl” refers to —CH₂COSCH₃, —CH₂COSCH₂CH₃. The“haloalkylthiocarbonylalkyl” refers to —CH₂COSCF₃, —CH₂COSCH₂CF₃.The “alkylcarbonyloxy” such as —OCOCH₃. The “haloalkylcarbonyloxy” suchas —OCOCF₃.The “alkoxycarbonyloxy” such as —OCOOCH₃. The “haloalkoxycarbonyloxy”such as —OCOOCF₃. The “alkoxyalkoxy” stands for —OCH₂OCH₃. The“haloalkoxyalkoxy” stands for —OCH₂OCF₃. The “alkoxycarbonylalkoxy”stands for —OCH₂COOCH₃. The “alkylsulfonylaminocarbonyl” refers toalkyl-SO₂—NH—CO—.The “alkylcarbonylamino” refers to alkyl-CO—NH—. The“cycloalkyloxycarbonyl” means cyclopropyloxycarbonyl,cyclohexyloxycarbonyl. The “alkoxycarbonylalkoxy” stands for—OCH₂COOCF₃. The “alkylsulfonyloxy” such as alkyl-O—SO₂CH₃. The“haloalkylsulfonyloxy” such as —O—SO₂CF₃. The “alkylaminocarbonyloxy”such as —O—CONHCH₃. The “haloalkylaminocarbonyloxy” such as —O—CONHCF₃.The “aryl” in (hetero)arylcarbonylalkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, (hetero)arylalkyloxycarbonyl and(hetero)arylalkyl includes phenyl or naphthyl etc. The “heteroaryl”stands for five member ring or six member ring containing one or more N,O, S hetero atoms, such as furyl, pyrazolyl, thiazolyl, pyridinyl,pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, quinolinyl, etc.(Hetero)arylcarbonylalkyl refers to —CH₂COPh, etc.(Hetero)aryloxycarbonyl such as phenoxycarbonyl,p-chlorophenoxycarbonyl, p-nitrophenoxycarbonyl, naphthyloxycarbonyl,etc. Arylalkyloxycarbonyl means benzyloxycarbonyl,p-chlorobenzyloxycarbonyl, p-trifluoromethylbenzyloxycarbonyl, etc.

(Hetero)arylcarbonyl refers to benzoyl, 4-C₁-benzoyl, etc.(Hetero)arylalkyloxycarbonyl refers to —COOCH₂Ph, —COOCH₂-4-Cl-Ph, etc.

(Hetero)arylalkyl means benzyl, phenylethyl, 4-chloro-benzyl,2-chloro-5-picolyl, 2-chloro-5-methylthiazole, etc.

The present invention is also explained by the following compoundshaving a structure as represented by formula I listed in Table 1 toTable 118, but without being restricted thereby.

Table 1: in general formula I-A, R₁=CH₃, R₂=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ refers to Table 1, therepresentative compounds are coded as I-1-I-58.

TABLE 1 No. R₉ I-1 H I-2 F I-3 Cl I-4 Br I-5 I I-6 CH₃ I-7 Et I-8 n-PrI-9 i-Pr I-10 n-Bu I-11 s-Bu I-12 t-Bu I-13 CH₂F I-14 CH₂Cl I-15 CH₂BrI-16 CHF₂ I-17 CHCl₂ I-18 CHBr₂ I-19 CClF₂ I-20 CCl₃ I-21 CBr₃ I-22 CF₃I-23 CN I-24 CH₂OCH₃ I-25 CH₂OCH₂CF₃ I-26 CH₂N(CH₃)₂ I-27 CH₂CN I-28OCH₃ I-29 OCF₃ I-30 OCH₂CF₃ I-31 SCH₃ I-32 SO₂CH₃ I-33 CO₂H I-34 CO₂CH₃I-35 CO₂C₂H₅ I-36 CO₂CH₂CF₃ I-37 CO₂-t-Bu I-38 CONH₂ I-39 CONHCH₃ I-40CON(CH₃)₂ I-41 CON(CH₃)₂ I-42 CONHNHCH₃ I-43 CONHN(CH₃)₂ I-44 CONHOCH₃I-45 CONHNH₂ I-46 CON(CH₃)NH₂ I-47 CONHNHCOCH₃ I-48 CONHNHCO₂CH₃ I-49CONHNH-Ph I-50 NO₂ I-51 NH₂ I-52 NHCH₃ I-53 NHCH₂CH₃ I-54 NHCOCH₃ I-55NHCO₂CH₃ I-56 NHSO₂CH₃ I-57 NHSO₂CF₃ I-58 N(CH₃)SO₂CH₃

Table 2: in general formula I-A, R₁=CH₃, R₂=R_(5b)=Cl,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-59-I-116.

Table 3: in general formula I-A, R₁=CH₃, R₂=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-117-I-174.

Table 4: in general formula I-A, R₁=CH₃, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-175-I-232.

Table 5: in general formula I-A, R₁=C₂H₅, R₂=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-233-I-290.

Table 6: in general formula I-A, R₁=C₂H₅, R₂=R_(5b)=Cl,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-291-I-348.

Table 7: in general formula I-A, R₁=C₂H₅, R₂=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-349-I-406.

Table 8: in general formula I-A, R₁=C₂H₅, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-407-I-464.

Table 9: in general formula I-A, R₁=CH₃, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-465-I-522.

Table 10: in general formula I-A, R₁=CH₃, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-523-I-580.

Table 11: in general formula I-A, R₁=C₂H₅, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-581-I-638.

Table 12: in general formula I-A, R₁=C₂H₅, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-639-I-696.

Table 13: in general formula I-A, R₁=CH₃, R₂=R₈=R₁₁=Cl,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-697-I-754.

Table 14: in general formula I-A, R₁=CH₃, R₂=R₈=R₁₀=R₁₁=Cl,R₃=R₄=R_(5b)=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-755-I-812.

Table 15: in general formula I-A, R₁=C₂H₅, R₂=R₈=R₁=Cl,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-813-I-870.

Table 16: in general formula I-A, R₁=C₂H₅, R₂=R₈=R₁₀=R₁₁=Cl,R₃=R₄=R_(5b)=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-871-I-928.

Table 17: in general formula I-A, R₁=CH₃, R₂=Cl, R₁₁=CF₃,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-929-I-986.

Table 18: in general formula I-A, R₁=C₂H₅, R₂=Cl, R₁₁=CF₃,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-987-I-1044.

Table 19: in general formula I-A, R₁=CH₃, R₂=Cl, R₁₁=CO₂CH₃,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1045-I-1102.

Table 20: in general formula I-A, R₁=CH₃, R₂=Cl, R₁₁=CONH₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1103-I-1160.

Table 21: in general formula I-A, R₁=CH₃, R₂=Cl, R₁=CONHCH₃,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1161-I-1218.

Table 22: in general formula I-A, R₁=C₂H₅, R₂=Cl, R₁₁=CO₂CH₃,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1219-I-1276.

Table 23: in general formula I-A, R₁=C₂H₅, R₂=Cl, R₁=CONH₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1277-I-1334.

Table 24: in general formula I-A, R₁=C₂H₅, R₂=Cl, R₁₁=CONHCH₃,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1335-I-1392.

Table 25: in general formula I-A, R₁=CH₃, R₂=R_(5b)=R₁₁=Cl,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-1393-I-1450.

Table 26: in general formula I-A, R₁=C₂H₅, R₂=R_(5b)=R₁₁=Cl,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-1451-I-1508.

Table 27: in general formula I-A, R₁=CH₃, R₂=R₁₁=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-1509-I-1566.

Table 28: in general formula I-A, R₁=C₂H₅, R₂=R₁₁=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-1567-I-1624.

Table 29: in general formula I-A, R₁=CH₃, R₂=R₁=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-1625-I-1682.

Table 30: in general formula I-A, R₁=C₂H₅, R₂=R₁=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-1683-I-1740.

Table 31: in general formula I-A, R₁=CH₃, R₂=Br,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1741-I-1798.

Table 32: in general formula I-A, R₁=C₂H₅, R₂=Br,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1799-I-1856.

Table 33: in general formula I-A, R₁=CH₃, R₂=Br, R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1857-I-1914.

Table 34: in general formula I-A, R₁=C₂H₅, R₂=Br, R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1915-I-1972.

Table 35: in general formula I-A, R₁=CH₃, R₂=Br, R_(5b)=Cl,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-1973-I-2030.

Table 36: in general formula I-A, R₁=C₂H₅, R₂=Br, R_(5b)=Cl,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2031-I-2088.

Table 37: in general formula I-A, R₁=CH₃, R₂=R_(5b)=Br,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2089-I-2146.

Table 38: in general formula I-A, R₁=C₂H₅, R₂=R_(5b)=Br,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2147-I-2204.

Table 39: in general formula I-A, R₁=CH₃, R₂=Br, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2205-I-2262.

Table 40: in general formula I-A, R₁=C₂H₅, R₂=Br, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2263-I-2320.

Table 41: in general formula I-A, R₁=CF₂H, R₂=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2321-I-2378.

Table 42: in general formula I-A, R₁=CF₂H, R₂=R_(5b)=Cl,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2379-I-2436.

Table 43: in general formula I-A, R₁=CF₂H, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2437-I-2494.

Table 44: in general formula I-A, R₁=CF₂H, R₂=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2495-I-2552.

Table 45: in general formula I-A, R₁=CF₂H, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2553-I-2610.

Table 46: in general formula I-A, R₁=CF₂H, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2611-I-2668.

Table 47: in general formula I-A, R₁=CF₂H, R₂=R₁₁=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-2669-I-2726.

Table 48: in general formula I-A, R₁=CF₃, R₂=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2727-I-2784.

Table 49: in general formula I-A, R₁=CF₃, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2785-I-2842.

Table 50: in general formula I-A, R₁=CF₃, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2843-I-2900.

Table 51: in general formula I-A, R₁=CH₂Cl, R₂=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2901-I-2958.

Table 52: in general formula I-A, R₁=CH₂Cl, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-2959-I-3016.

Table 53: in general formula I-A, R₁=CH₂Cl, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-3017-I-3074.

Table 54: in general formula I-B, R₁=CH₃, R₂=Cl, R₃=R₄=R_(5b)=R₁₀=R₁₁=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3075-I-3132.

Table 55: in general formula I-B, R₁=CH₃, R₂=R_(5b)=Cl, R₃=R₄=R₁₀=R₁₁=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3133-I-3190.

Table 56: in general formula I-B, R₁=CH₃, R₂=Cl, R_(5b)=Br,R₃=R₄=R₁₀=R₁₁=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3191-I-3248.

Table 57: in general formula I-B, R₁=CH₃, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₁₀=R₁₁=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3249-I-3306.

Table 58: in general formula I-B, R₁=C₂H₅, R₂=Cl,R₃=R₄=R_(5b)=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-3307-I-3364.

Table 59: in general formula I-B, R₁=C₂H₅, R₂=R_(5b)=Cl,R₃=R₄=R₁₀=R₁₁=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3365-I-3422.

Table 60: in general formula I-B, R₁=C₂H₅, R₂=Cl, R_(5b)=Br,R₃=R₄=R₁₀=R₁₁=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3423-I-3480.

Table 61: in general formula I-B, R₁=C₂H₅, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₁₀=R₁₁=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3481-I-3538.

Table 62: in general formula I-B, R₁=CH₃, R₂=R₁₁=Cl, R₃=R₄=R_(5b)=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3539-I-3596.

Table 63: in general formula I-B, R₁=CH₃, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-3597-I-3654.

Table 64: in general formula I-B, R₁=C₂H₅, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-3655-I-3712.

Table 65: in general formula I-B, R₁=C₂H₅, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-3713-I-3770.

Table 66: in general formula I-B, R₁=CH₃, R₂=R₁₀=Cl, R₃=R₄=R_(5b)=R₁₁=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3771-I-3828.

Table 67: in general formula I-B, R₁=CH₃, R₂=R₁₀=R₁₁=Cl, R₃=R₄=R_(5b)=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3829-I-3886.

Table 68: in general formula I-B, R₁=C₂H₅, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-3887-I-3944.

Table 69: in general formula I-B, R₁=C₂H₅, R₂=R₁₀=R₁₁=Cl,R₃=R₄=R_(5b)=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-3945-I-4002.

Table 70: in general formula I-B, R₁=CH₃, R₂=Cl, R₁₁=CF₃,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-4003-I-4060.

Table 71: in general formula I-B, R₁=C₂H₅, R₂=Cl, R₁₁=CF₃,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-4061-I-4118.

Table 72: in general formula I-B, R₁=CH₃, R₂=Br, R₃=R₄=R_(5b)=R₁₀=R₁₁=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4119-I-4176.

Table 73: in general formula I-B, R₁=C₂H₅, R₂=Br,R₃=R₄=R_(5b)=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-4177-I-4234.

Table 74: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=R₄=R_(5b)=R₈=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4235-I-4292.

Table 75: in general formula I-C, R₁=CH₃, R₂=R_(5b)=Cl, R₃=R₄=R₈=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4293-I-4350.

Table 76: in general formula I-C, R₁=CH₃, R₂=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4351-I-4408.

Table 77: in general formula I-C, R₁=CH₃, R₂=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4409-I-4466.

Table 78: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₃=R₄=R_(5b)=R₈=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4467-I-4524.

Table 79: in general formula I-C, R₁=C₂H₅, R₂=R_(5b)=Cl, R₃=R₄=R₈=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4525-I-4582.

Table 80: in general formula I-C, R₁=C₂H₅, R₂=Cl, R_(5b)=Br,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4583-I-4640.

Table 81: in general formula I-C, R₁=C₂H₅, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₈=R₁₀=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4641-I-4698.

Table 82: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=R₄=R_(5b)=H,R₈=R₁₀=CH₃, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4699-I-4756.

Table 83: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=R₄=R_(5b)=H,R₈=R₁₀=OCH₃, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4757-I-4814.

Table 84: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=R₄=R_(5b)=H,R₈=R₁₀=Cl, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4815-I-4872.

Table 85: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=CH₃,R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-4873-I-4930.

Table 86: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=CH₃, R₄=R_(5b)=H,R₈=R₁₀=CH₃, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4931-I-4988.

Table 87: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=CH₃, R₄=R_(5b)=H,R₈=R₁₀=OCH₃, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-4989-I-5046.

Table 88: in general formula I-C, R₁=CH₃, R₂=Cl, R₃=CH₃, R₄=R_(5b)=H,R₈=R₁₀=Cl, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-5047-I-5104.

Table 89: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₃=CH₃,R₄=R_(5b)=R₈=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5105-I-5162.

Table 90: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₃=R₄=R_(5b)=H,R₈=R₁₀=CH₃, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-5163-I-5220.

Table 91: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₃=R₄=R_(5b)=H,R₈=R₁₀=OCH₃, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-5221-I-5278.

Table 92: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₃=R₄=R_(5b)=H,R₈=R₁₀=Cl, the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-5279-I-5336.

Table 93: in general formula I-C, R₁=CH₃, R₂=R₈=Cl, R₃=R₄=R_(5b)=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-5337-I-5394.

Table 94: in general formula I-C, R₁=CH₃, R₂=Cl, R₈=CH₃,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5395-I-5452.

Table 95: in general formula I-C, R₁=CH₃, R₂=Cl, R₈=OCH₃,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5453-I-5510.

Table 96: in general formula I-C, R₁=C₂H₅, R₂=R₈=Cl, R₃=R₄=R_(5b)=R₁₀=H,the substituent R₉ are consistent with those in Table 1 andcorresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-5511-I-5568.

Table 97: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₈=CH₃,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5569-I-5626.

Table 98: in general formula I-C, R₁=C₂H₅, R₂=Cl, R₈=OCH₃,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5627-I-5684.

Table 99: in general formula I-D, R₁=CH₃, R₂=Cl,R₃=R₄=R_(5b)=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5685-I-5742.

Table 100: in general formula I-D, R₁=CH₃, R₂=R_(5b)=Cl,R₃=R₄=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5743-I-5800.

Table 101: in general formula I-D, R₁=CH₃, R₂=Cl, R_(5b)=Br,R₃=R₄=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5801-I-5858.

Table 102: in general formula I-D, R₁=CH₃, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5859-I-5916.

Table 103: in general formula I-D, R₁=C₂H₅, R₂=Cl,R₃=R₄=R_(5b)=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with thosein Table 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5917-I-5974.

Table 104: in general formula I-D, R₁=C₂H₅, R₂=R_(5b)=Cl,R₃=R₄=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-5975-I-6032.

Table 105: in general formula I-D, R₁=C₂H₅, R₂=Cl, R_(5b)=Br,R₃=R₄=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6033-I-6090.

Table 106: in general formula I-D, R₁=C₂H₅, R₂=Cl, R_(5b)=OCH₃,R₃=R₄=R₇=R₁₀=R₁₁=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6091-I-6148.

Table 107: in general formula I-D, R₁=CH₃, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₇=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6149-I-6206.

Table 108: in general formula I-D, R₁=CH₃, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₇=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6207-I-6264.

Table 109: in general formula I-D, R₁=C₂H₅, R₂=R₁₁=Cl,R₃=R₄=R_(5b)=R₇=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6265-I-6322.

Table 110: in general formula I-D, R₁=C₂H₅, R₂=Cl, R₁₁=NO₂,R₃=R₄=R_(5b)=R₇=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6323-I-6380.

Table 111: in general formula I-D, R₁=CH₃, R₂=R₇=R₁₁=Cl,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6381-I-6438.

Table 112: in general formula I-D, R₁=CH₃, R₂=R₇=R₁₀=R₁₁=Cl,R₃=R₄=R_(5b)=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-6439-I-6496.

Table 113: in general formula I-D, R₁=C₂H₅, R₂=R₇=R₁₁=Cl,R₃=R₄=R_(5b)=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6497-I-6554.

Table 114: in general formula I-D, R₁=C₂H₅, R₂=R₇=R₁₀=R₁₁=Cl,R₃=R₄=R_(5b)=H, the substituent R₉ are consistent with those in Table 1and corresponding to I-1-I-58 in table 1 in turn, the representativecompounds are coded as I-6555-I-6612.

Table 115: in general formula I-D, R₁=CH₃, R₂=Cl, R₁₁=CF₃,R₃=R₄=R_(5b)=R₇=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6613-I-6670.

Table 116: in general formula I-D, R₁=C₂H₅, R₂=Cl, R₁₁=CF₃,R₃=R₄=R_(5b)=R₇=R₁₀=H, the substituent R₉ are consistent with those inTable 1 and corresponding to I-1-I-58 in table 1 in turn, therepresentative compounds are coded as I-6671-I-6728.

Table 117: the salts of some compounds having a structure as representedby formula I of the present invention are listed in Table 117, butwithout being restricted thereby.

TABLE 117 the salts of some compounds No. structure I-6729

I-6730

I-6731

I-6732

I-6733

I-6734

I-6735

I-6736

I-6737

I-6738

I-6739

I-6740

I-6741

I-6742

I-6743

I-6744

I-6745

I-6746

I-6747

I-6748

I-6749

I-6750

I-6751

I-6752

I-6753

I-6754

I-6755

I-6756

I-6757

I-6758

I-6759

I-6760

I-6761

I-6762

I-6763

I-6764

I-6765

I-6766

I-6767

I-6768

I-6769

I-6770

I-6771

I-6772

I-6773

I-6774

I-6775

I-6776

I-6777

I-6778

I-6779

I-6780

I-6781

I-6782

Some compounds represented by general formula I-E, I-F, I-G and I-H ofthe present invention are listed in Table 118, but without beingrestricted thereby.

TABLE 118 No. structure I-6783

I-6784

I-6785

I-6786

I-6787

I-6788

I-6789

I-6790

I-6791

I-6792

I-6793

I-6794

I-6795

I-6796

I-6797

I-6798

I-6799

I-6800

I-6801

I-6802

I-6803

I-6804

I-6805

I-6806

I-6807

I-6808

I-6809

I-6810

I-6811

I-6812

I-6813

I-6814

I-6815

I-6816

I-6817

I-6818

I-6819

I-6820

I-6821

I-6822

I-6823

I-6824

I-6825

I-6826

I-6827

I-6828

I-6829

I-6830

I-6831

I-6832

I-6833

I-6834

I-6835

I-6836

I-6837

I-6838

I-6839

I-6840

I-6841

I-6842

I-6843

I-6844

I-6845

I-6846

In the general formula I, A=NR₁₂, R₁₂≠H, part of preferred substituentsof R₁₂ are listed in table 119, but without being restricted thereby.The present invention is also explained by the following compounds inthe general formula I listed in Table 120, but without being restrictedthereby.

TABLE 119 R₁₂ substituents R₁₂ OH C₂H₅ i-C₄H₉ CHF₂ CHCl₂ OC₂H₅ OCH₂CF₃SCH₃ CH₂CH═CH₂ CH₂C≡C—I CH₂CH₂OCH₂CH₃ CH₂SCH₃ CH₂SCH₂Cl SOC₂H₅ SO₂C₂H₅SO₂NHCH₃ COC₂H₅ CO-i-C₄H₉ COOCH₃ COOCF₃ CH₂COOC₂H₅ CONHC₂H₅ COOCH₂CH═CH₂SNHCH₃

—C(═O)H n-C₃H₇ t-C₄H₉ CHBr₂ CCl₃ OCH(CH₃)₂ OCF₂CF₃ SC₂H₅ CH₂CH═CCl₂CH₂OCH₃ CH₂OCH₂Cl CH₂SCH₂CH₃ CH₂SCH₂CH₂Cl SOCF₃ SO₂CF₃ SO₂N(CH₃)₃CO-n-C₃H₇ CO-t-C₄H₉ COOC₂H₅ COOCH₂CH₂Cl CH₂COCH₃ CONH-t-C₄H₉ COOCH₂C≡CHSNHC₂H₅

CBr₃ i-C₃H₇ CI₃ CF₃ CH₂F OC(CH₃)₃ OCH₂F SCH₂CH═CH₂ C≡CH CH₂OCH₂CH₃CH₂OCH₂CH₂Cl CH₂CH₂SCH₃ CH₂CH₂SCH₂Cl SOCH₂CF₃ SO₂CH₂CF₃ CONHSO₂CH₃CO-i-C₃H₇ COCF₃ COO-n-C₃H₇ COOCH₂CF₃ CH₂COC₂H₅ CON(CH₃)₂ COOCH₂OCH₃SN(CH₃)₂

CH₃ n-C₄H₉ CH₂Br CH₂Cl OCH₃ OCF₃ OCHF₂ CH═CH₂ CH₂C≡CH CH₂CH₂OCH₃CH₂CH₂OCH₂Cl CH₂CH₂SCH₂CH₃ SOCH₃ SO₂CH₃ SO₂NHCOCH₃ COCH₃ CO-n-C₄H₉COCH₂Cl COO-t-C₄H₉ CH₂COOCH₃ CONHCH₃ CON(C₂H₅)₂ COOCH₂CH₂OCH₃ SN(C₂H₅)₂

TABLE 120 No. structure I-6847

I-6848

I-6849

I-6850

I-6851

I-6852

I-6853

I-6854

I-6855

I-6856

I-6857

I-6858

I-6859

I-6860

I-6861

I-6862

I-6863

I-6864

I-6865

I-6866

I-6867

I-6868

I-6869

I-6870

I-6871

I-6872

I-6873

I-6874

I-6875

I-6876

I-6877

I-6878

I-6879

I-6880

I-6881

I-6882

I-6883

I-6884

I-6885

I-6886

I-6887

I-6888

I-6889

I-6890

I-6891

I-6892

I-6893

I-6894

In the general formula II, part of preferred substituents of R₁, R₂,R₃(R₄), R_(5a)(R_(5b), R_(5c)), R₆(R₇, R₈, R₉, R₁₀, R₁₁) and R₁₂ areseparately listed in table 121, table 122, table 123, table 124, table125 and table 126, but without being restricted thereby.

TABLE 121 R₁ substituents R₁ CH₃ n-C₄H₉ CF₃ CH₂Br CF₂H

C₂H₅ s-C₄H₉ CCl₃ CClF₂ CBr₂H

n-C₃H₇ i-C₄H₉ CH₂F CFCl₂ CBr₃

i-C₃H₇ t-C₄H₉ CH₂Cl CCl₂H CClBr₂

TABLE 122 R₂ substituents R₂ R₂ R₂ R₂ F Cl Br I CN OCH₃ OC₂H₅ OC₃H₇-nOC₃H₇-i OC₄H₉-n OC₄H₉-i OC₄H₉-t

TABLE 123 R₃(R₄) substituents R₃(R₄) H i-C₃H₇ F t-C₄H₉ OCH₃ CH₃ n-C₄H₉Cl

OC₂H₅ C₂H₅ s-C₄H₉ Br

OC₃H₇-n n-C₃H₇ i-C₄H₉ I

OC₃H₇-i CR₃(R₄)

TABLE 124 R_(5a) (R_(5b), R_(5c)) substituents R_(5a) (R_(5b), R_(5c))R_(5a) (R_(5b), R_(5c)) R_(5a) (R_(5b), R_(5c)) R_(5a) (R_(5b), R_(5c))H CH₃ i-C₄H₉ OC₄H₉-n F C₂H₅ t-C₄H₉ OC₄H₉-i Cl n-C₃H₇ OCH₃ OC₄H₉-t Bri-C₃H₇ OC₂H₅ OCF₃ I n-C₄H₉ OC₃H₇-n OCH₂CF₃ OH s-C₄H₉ OC₃H₇-i OCF₂CF₃

TABLE 125 R₆ (R₇, R₈, R₉, R₁₀, R₁₁) substituents R₆ (R₇, R₈, R₉, R₁₀, R₆(R₇, R₈, R₆ (R₇, R₈, R₉, R₆ (R₇, R₈, R₉, R₁₁) R₉, R₁₀, R₁₁) R₁₀, R₁₁)R₁₀, R₁₁) R₆ (R₇, R₈, R₉, R₁₀, R₁₁) H 4-CH₃ 3-CH₂OCH₃ 2,6-2Cl-4-CONH₂2-CF₃-4-Br-6-NO₂ 2-F 2,3-2CH₃ 4-CH₂OCH₃ 2,4-2Cl-6-NO₂ 3-NO₂-4-CF₃ 3-F2,4-2CH₃ 2-OCOCH₃ 2,4-2Cl-6-CN 2-NO₂-4-CN-5-CF₃ 4-F 2,5-2CH₃ 3-OCOCH₃2,4-2Cl-6-CF₃ 2-NO₂-4-CF₃-5-CN 2,3-2F 2,6-2CH₃ 4-OCOCH₃ 2,4-2F-6-NO₂4-OCF₃-2,6-2Br 2,4-2F 3,4-2CH₃ 2-OCOCH₂CH₃ 2,6-2F-4-NO₂2-CH₃-4-Cl-5-CH₂CO₂C₂H₅ 2,5-2F 3,5-2CH₃ 3-OCOCH₂CH₃ 2-NO₂-4-F2,4-2Cl-3-CH₃ 2,6-2F 2-C₂H₅ 4-OCOCH₂CH₃ 2-NO₂-4-Br 2,4-2Cl-3-CH₃-6-NO₂3,4-2F 3-C₂H₅ 2-OCO₂CH₃ 2-NO₂-4-CF₃ 2-Cl-3-CH₃ 3,5-2F 4-C₂H₅ 3-OCO₂CH₃2-NO₂-4-CN 2-CH₃-3-Cl 2,3,4-3F 2-CF₃ 4-OCO₂CH₃ 2-NO₂-4-COCH₃2-CH₃-3-Cl-4,6-2NO₂ 2,3,5-3F 3-CF₃ 2-OCH₂OCH₃ 2-NO₂-4-CONH₂2-CH₃-3-Cl-4-NO₂ 2,4,5-3F 4-CF₃ 3-OCH₂OCH₃ 2-NO₂-4-CH₃ 2-CH₃-3-Cl-6-NO₂2,3,6-3F 2-OCH₃ 4-OCH₂OCH₃ 2-NO₂-4-OCH₃ 2-Cl-3-CH₃-4,6-2NO₂ 2,4,6-3F3-OCH₃ 2-OCF₂OCF₃ 2-NO₂-4-SCH₃ 2-Cl-3-CH₃-4-NO₂ 3,4,5-3F 4-OCH₃3-OCF₂OCF₃ 2-NO₂-4-NCH₃ 2-Cl-3-CH₃-6-NO₂ 2-Cl 2-SCH₃ 4-OCF₂OCF₃2-F-4-NO₂ 2-Br-4-NO₂-6-CN 3-Cl 3-SCH₃ 2-COPh 2-Br-4-NO₂3-Cl-4-CF₃-2,6-2NO₂ 4-Cl 4-SCH₃ 3-COPh 2-CF₃-4-NO₂ 2NO₂-4,5-2Cl 2,3-2Cl2-OCF₃ 4-COPh 2-CN-4-NO₂ 2-NO₂-3,5-2Cl 2,4-2Cl 3-OCF₃ 2-COCH₂Ph2-COCH₃-4-NO₂ 2,5-2Cl-4-NO₂ 2,5-2Cl 4-OCF₃ 3-COCH₂Ph 2-CONH₂-4-NO₂2,5-2Cl-6-NO₂ 2,6-2Cl 2-SCF₃ 4-COCH₂Ph 2-CH₃-4-NO₂ 2,3-2Cl-4-NO₂ 3,4-2Cl3-SCF₃ 2-NHPh 2-Cl-4-F-6-NO₂ 2,3-2Cl-6-NO₂ 3,5-2Cl 4-SCF₃ 3-NHPh2-Cl-4-Br-6-NO₂ 3,4-2Cl-2,6-2NO₂ 2,3,4-3Cl 2-OC₂H₅ 4-NHPh2-Cl-4-CH₃-6-NO₂ 2,5-2Cl-4,6-2NO₂ 2,3,5-3Cl 3-OC₂H₅ 2-OPh2-Cl-4-CF₃-6-NO₂ 2,4,5-3Cl-6-NO₂ 2,4,5-3Cl 4-OC₂H₅ 3-OPh 2-Cl-4,6-2NO₂2,3,4-3Cl-5-NO₂ 2,3,6-3Cl 2-NHCH₃ 4-OPh 2-Cl-4-CN-6-NO₂ 2,3,4-3Cl-6-NO₂2,4,6-3Cl 3-NHCH₃ 2-CONHPh 2-Cl-4-OCF₃-6-NO₂ 2,3,5-3Cl-4,6-2CN 3,4,5-3Cl4-NHCH₃ 3-CONHPh 2-F-4-Cl-6-NO₂ 2,5-2Cl-4-OCF₂OCF₃ 2-Br 2-N(CH₃)₂4-CONHPh 2-Br-4-Cl-6-NO₂ 2,6-2Br-4-NO₂ 3-Br 3-N(CH₃)₂ 2-CO₂Ph2-CH₃-4-Cl-6-NO₂ 2-F-4-NO₂-6-Cl 4-Br 4-N(CH₃)₂ 3-CO₂Ph 2-CF₃-4-Cl-6-NO₂2-Cl-4-NO₂-6-SCN 2,3-2Br 2-COCH₃ 4-CO₂Ph 4-Cl-2,6-2NO₂ 2-Br-4-NO₂-6-Cl2,4-2Br 3-COCH₃ 2-CONH₂ 2-F-4-CN 2-Cl-4-NO₂-6-OCH₃ 2,5-2Br 4-COCH₃3-CONH₂ 2-CN-4-CF₃ 2-Cl-4-NO₂-6-SCH₃ 2,6-2Br 2-COC₂H₅ 4-CONH₂4-CF₃-2,6-2NO₂ 2-Cl-4-NO₂-6-NHCH₃ 3,4-2Br 3-COC₂H₅ 2-Cl-4-F4-CN-2,6-2NO₂ 2-Cl-4-NO₂-6-SO₂CH₃ 3,5-2Br 4-COC₂H₅ 2-Cl-4-Br4-CH₃-2,6-2NO₂ 2-Cl-4-SO₂CH₃ 2,3,4-3Br 2-SO₂CH₃ 2-Cl-4-CH₃4-OCF₃-2,6-2NO₂ 2,6-2Cl-4-SO₂CH₃ 2,3,5-3Br 3-SO₂CH₃ 2-Cl-4-CF₃4-OCH₃-2,6-2NO₂ 2,6-2Cl-4-CH₃ 2,4,5-3Br 4-SO₂CH₃ 2-Cl-4-NO₂4-SCH₃-2,6-2NO₂ 2,6-2Cl-4-CO₂CH₃ 2,3,6-3Br 2-OCHF₂ 2-Cl-4-CN4-NHCH₃-2,6-2NO₂ 2,6-2Cl-4-CONHCH₃ 2,4,6-3Br 3-OCHF₂ 2-Cl-4-OCF₃4-F-2,6-2NO₂ 2,6-2Cl-4-CON(CH₃)₂ 3,4,5-3Br 4-OCHF₂ 2-F-4-Cl2-CF₃-4,6-2NO₂ 2,6-2Cl-4-CF(CF₃)₂ 2-CN 2-SO₂C₂H₅ 2-Br-4-Cl 2-CN-4,6-2NO₂2-Cl-4-CF(CF₃)₂-6-Br 3-CN 3-SO₂C₂H₅ 2-CH₃-4-Cl 2-CH₃-4,6-2NO₂2-F-4-CF(CF₃)₂-6-Br 4-CN 4-SO₂C₂H₅ 2-CF₃-4-Cl 2-F-4,6-2NO₂2-F-4-CF(CF₃)₂-6-Cl 2-NO₂ 2-CO₂CH₃ 2-NO₂-4-Cl 2-OCF₃-4,6-2NO₂2,4,5-3Cl-3,6-2CN 3-NO₂ 3-CO₂CH₃ 2-CN-4-Cl 2-CF₃-4-Br 2,3,5-3F-4,6-2CN4-NO₂ 4-CO₂CH₃ 2-OCF₃-4-Cl 3-CF₃-4-NO₂ 2-SO₂NH₂ 2,4-2NO₂ 2-CO₂C₂H₅2,6-2Cl-4-NO₂ 2-CN-4-Cl-6-NO₂ 3-SO₂NH₂ 2,4,6-3NO₂ 3-CO₂C₂H₅2,6-2Cl-4-CF₃ 2-OCF₃-4-Cl-6-NO₂ 4-SO₂NH₂ 2-CH₃ 4-CO₂C₂H₅ 2,6-2Cl-4-CN3-CF₃-4-CN 3-CH₃ 2-CH₂OCH₃ 2,6-2Cl-4-COCH₃ 3-CN-4-CF₃

TABLE 126 R₁₂ substituents R₁₂ R₁₂ R₁₂ R₁₂ H OH CH₃ C₂H₅ n-C₃H₇ i-C₃H₇n-C₄H₉ s-C₄H₉ i-C₄H₉ t-C₄H₉ HCO CH₃CO CH₃CH₂CO n-C₃H₇CO i-C₃H₇CO CH₃SO₂CH₃CH₂SO₂ n-C₃H₇SO₂ n-C₄H₉SO₂

The present invention is also explained by the following compoundshaving a structure as represented by formula II listed in Table 127 toTable 202, Compounds having a structure as represented by formula II-Aare listed in Table 127 to Table 190, Compounds having a structure asrepresented by formula II-B are listed in Table 191 to Table 201, butwithout being restricted thereby.

In general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=R₄=R_(5b)=H, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ refer to Table 127, therepresentative compounds are coded as II-1-II-2780

TABLE 127 No. R₇ R₈ R₉ R₁₀ R₁₁ II-1 H H H H H II-2 F H H H H II-3 H F HH H II-4 H H F H H II-5 F F H H H II-6 F H F H H II-7 F H H F H II-8 F HH H F II-9 H F F H H II-10 H F H F H II-11 F F F H H II-12 F F H F HII-13 F H F F H II-14 F F H H F II-15 F H F H F II-16 H F F F H II-17 ClH H H H II-18 H Cl H H H II-19 H H Cl H H II-20 Cl Cl H H H II-21 Cl HCl H H II-22 Cl H H Cl H II-23 Cl H H H Cl II-24 H Cl Cl H H II-25 H ClH Cl H II-26 Cl Cl Cl H H II-27 Cl Cl H Cl H II-28 Cl H Cl Cl H II-29 ClCl H H Cl II-30 Cl H Cl H Cl II-31 H Cl Cl Cl H II-32 Br H H H H II-33 HBr H H H II-34 H H Br H H II-35 Br Br H H H II-36 Br H Br H H II-37 Br HH Br H II-38 Br H H H Br II-39 H Br Br H H II-40 H Br H Br H II-41 Br BrBr H H II-42 Br Br H Br H II-43 Br H Br Br H II-44 Br Br H H Br II-45 BrH Br H Br II-46 H Br Br Br H II-47 CN H H H H II-48 H CN H H H II-49 H HCN H H II-50 NO₂ H H H H II-51 H NO₂ H H H II-52 H H NO₂ H H II-53 NO₂ HNO₂ H H II-54 NO₂ H NO₂ H NO₂ II-55 CH₃ H H H H II-56 H CH₃ H H H II-57H H CH₃ H H II-58 CH₃ CH₃ H H H II-59 CH₃ H CH₃ H H II-60 CH₃ H H CH₃ HII-61 CH₃ H H H CH₃ II-62 H CH₃ CH₃ H H II-63 H CH₃ H CH₃ H II-64 C₂H₅ HH H H II-65 H C₂H₅ H H H II-66 H H C₂H₅ H H II-67 CF₃ H H H H II-68 HCF₃ H H H II-69 H H CF₃ H H II-70 OCH₃ H H H H II-71 H OCH₃ H H H II-72H H OCH₃ H H II-73 SCH₃ H H H H II-74 H SCH₃ H H H II-75 H H SCH₃ H HII-76 OCF₃ H H H H II-77 H OCF₃ H H H II-78 H H OCF₃ H H II-79 SCF₃ H HH H II-80 H SCF₃ H H H II-81 H H SCF₃ H H II-82 OC₂H₅ H H H H II-83 HOC₂H₅ H H H II-84 H H OC₂H₅ H H II-85 NHCH₃ H H H H II-86 H NHCH₃ H H HII-87 H H NHCH₃ H H II-88 N(CH₃)₂ H H H H II-89 H N(CH₃)₂ H H H II-90 HH N(CH₃)₂ H H II-91 COCH₃ H H H H II-92 H COCH₃ H H H II-93 H H COCH₃ HH II-94 COC₂H₅ H H H H II-95 H COC₂H₅ H H H II-96 H H COC₂H₅ H H II-97SO₂CH₃ H H H H II-98 H SO₂CH₃ H H H II-99 H H SO₂CH₃ H H II-100 OCHF₂ HH H H II-101 H OCHF₂ H H H II-102 H H OCHF₂ H H II-103 SO₂C₂H₅ H H H HII-104 H SO₂C₂H₅ H H H II-105 H H SO₂C₂H₅ H H II-106 CO₂CH₃ H H H HII-107 H CO₂CH₃ H H H II-108 H H CO₂CH₃ H H II-109 CO₂C₂H₅ H H H HII-110 H CO₂C₂H₅ H H H II-111 H H CO₂C₂H₅ H H II-112 CH₂OCH₃ H H H HII-113 H CH₂OCH₃ H H H II-114 H H CH₂OCH₃ H H II-115 OCOCH₃ H H H HII-116 H OCOCH₃ H H H II-117 H H OCOCH₃ H H II-118 OCOCH₂CH₃ H H H HII-119 H OCOCH₂CH₃ H H H II-120 H H OCOCH₂CH₃ H H II-121 OCO₂CH₃ H H H HII-122 H H OCO₂CH₃ H H H II-123 H H OCO₂CH₃ H H II-124 OCH₂OCH₃ H H H HII-125 H OCH₂OCH₃ H H H II-126 H H OCH₂OCH₃ H H II-127 OCF₂OCF₃ H H H HII-128 H OCF₂OCF₃ H H H II-129 H H OCF₂OCF₃ H H II-130 COPh H H H HII-131 H COPh H H H II-132 H H COPh H H II-133 COCH₂Ph H H H H II-134 HCOCH₂Ph H H H II-135 H H COCH₂Ph H H II-136 NHPh H H H H II-137 H NHPh HH H II-138 H H NHPh H H II-139 OPh H H H H II-140 H OPh H H H II-141 H HOPh H H II-142 CONHPh H H H H II-143 H CONHPh H H H II-144 H H CONHPh HH II-145 CO₂Ph H H H H II-146 H CO₂Ph H H H II-147 H H CO₂Ph H H II-148CONH₂ H H H H II-149 H CONH₂ H H H II-150 H H CONH₂ H H II-151 Cl H F HH II-152 Cl H Br H H II-153 Cl H CH₃ H H II-154 Cl H CF₃ H H II-155 Cl HNO₂ H H II-156 Cl H CN H H II-157 Cl H OCF₃ H H II-158 F H Cl H H II-159Br H Cl H H II-160 CH₃ H Cl H H II-161 CF₃ H Cl H H II-162 NO₂ H Cl H HII-163 CN H Cl H H II-164 OCF₃ H Cl H H II-165 Cl H NO₂ H Cl II-166 Cl HCF₃ H Cl II-167 Cl H CN H Cl II-168 Cl H COCH₃ H Cl II-169 Cl H CONH₂ HCl II-170 Cl H Cl H NO₂ II-171 Cl H Cl H CN II-172 Cl H Cl H CF₃ II-173F H F H NO₂ II-174 F H NO₂ H F II-175 NO₂ H F H H II-176 NO₂ H Br H HII-177 NO₂ H CF₃ H H II-178 NO₂ H CN H H II-179 NO₂ H COCH₃ H H II-180NO₂ H CONH₂ H H II-181 NO₂ H CH₃ H H II-182 NO₂ H OCH₃ H H II-183 NO₂ HSCH₃ H H II-184 NO₂ H NCH₃ H H II-185 F H NO₂ H H II-186 Br H NO₂ H HII-187 CF₃ H NO₂ H H II-188 CN H NO₂ H H II-189 COCH₃ H NO₂ H H II-190CONH₂ H NO₂ H H II-191 CH₃ H NO₂ H H II-192 Cl H F H NO₂ II-193 Cl H BrH NO₂ II-194 Cl H CH₃ H NO₂ II-195 Cl H CF₃ H NO₂ II-196 Cl H NO₂ H NO₂II-197 Cl H CN H NO₂ II-198 Cl H OCF₃ H NO₂ II-199 F H Cl H NO₂ II-200Br H Cl H NO₂ II-201 CH₃ H Cl H NO₂ II-202 CF₃ H Cl H NO₂ II-203 NO₂ HCl H NO₂ II-204 F H CN H H II-205 CN H CF₃ H H II-206 NO₂ H CF₃ H NO₂II-207 NO₂ H CN H NO₂ II-208 NO₂ H CH₃ H NO₂ II-209 NO₂ H OCF₃ H NO₂II-210 NO₂ H OCH₃ H NO₂ II-211 NO₂ H SCH₃ H NO₂ II-212 NO₂ H NHCH₃ H NO₂II-213 NO₂ H F H NO₂ II-214 CF₃ H NO₂ H NO₂ II-215 CN H NO₂ H NO₂ II-216CH₃ H NO₂ H NO₂ II-217 F H NO₂ H NO₂ II-218 OCF₃ H NO₂ H NO₂ II-219 CF₃H Br H H II-220 H CF₃ NO₂ H H II-221 CN H Cl H NO₂ II-222 OCF₃ H Cl HNO₂ II-223 H CF₃ CN H H II-224 H CN CF₃ H H II-225 CF₃ H Br H NO₂ II-226H NO₂ CF₃ H H II-227 NO₂ H CN CF₃ H II-228 NO₂ H CF₃ CN H II-229 Br HOCF₃ H Br II-230 CH₃ H Cl CH₂CO₂C₂H₅ H II-231 Cl CH₃ Cl H OCF₂OCF₃II-232 Cl CH₃ Cl H NO₂ II-233 Cl CH₃ H H H II-234 CH₃ Cl H H H II-235CH₃ Cl NO₂ H NO₂ II-236 CH₃ Cl NO₂ H H II-237 CH₃ Cl H H NO₂ II-238 ClCH₃ NO₂ H NO₂ II-239 Cl CH₃ NO₂ H H II-240 Cl CH₃ H H NO₂ II-241 Br HNO₂ H CN II-242 NO₂ Cl CF₃ H NO₂ II-243 NO₂ H Cl Cl H II-244 NO₂ Cl H ClH II-245 Cl H NO₂ Cl H II-246 Cl H H Cl NO₂ II-247 Cl Cl NO₂ H H II-248Cl Cl H H NO₂ II-249 NO₂ Cl Cl H NO₂ II-250 Cl H NO₂ Cl NO₂ II-251 Cl HCl Cl NO₂ II-252 Cl Cl Cl NO₂ H II-253 Cl Cl Cl H NO₂ II-254 Cl Cl CN ClCN II-255 Cl H OCF₂OCF₃ Cl H II-256 Br H NO₂ H Br II-257 F H NO₂ H ClII-258 Cl H NO₂ H SCN II-259 Br H NO₂ H Cl II-260 Cl H NO₂ H OCH₃ II-261Cl H NO₂ H SCH₃ II-262 Cl H NO₂ H NHCH₃ II-263 Cl H NO₂ H SO₂CH₃ II-264Cl H SO₂CH₃ H H II-265 Cl H SO₂CH₃ H Cl II-266 Cl H CH₃ H Cl II-267 Cl HCO₂CH₃ H Cl II-268 Cl H CONHCH₃ H Cl II-269 Cl H CON(CH₃)₂ H Cl II-270Cl H CF(CF₃)₂ H Cl II-271 Cl H CF(CF₃)₂ H Br II-272 F H CF(CF₃)₂ H BrII-273 F H CF(CF₃)₂ H Cl II-274 Cl CN Cl Cl CN II-275 F F CN F CN II-276SO₂NH₂ H H H H II-277 H SO₂NH₂ H H H II-278 H H SO₂NH₂ H H

Table 128: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=R₄=R_(5b)=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-279-II-556.

Table 129: in general formula II-A, W=H, R₁=CH₃, R₂=R_(5b)=Cl, R₃=R₄=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-557-II-834.

Table 130: in general formula II-A, W=H, R₁=C₂H₅, R₂=R_(5b)=Cl, R₃=R₄=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-835-II-1112.

Table 131: in general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-1113-II-1390.

Table 132: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-1391-II-1668.

Table 133: in general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-1669-II-1946.

Table 134: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-1947-II-2224.

Table 135: in general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-2225-II-2502.

Table 136: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-2503-II-2780.

Table 137: in general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-2781-II-3058.

Table 138: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-3059-II-3336.

Table 139: in general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-3337-II-3614.

Table 140: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-3615-II-3892.

Table 141: in general formula II-A, W=H, R₁=CH₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-3893-II-4170.

Table 142: in general formula II-A, W=H, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-4171-II-4448.

Table 143: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl,R₃=R₄=R_(5b)=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-4449-II-4726.

Table 144: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl,R₃=R₄=R_(5b)=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-4727-II-5004.

Table 145: in general formula II-A, W=CH₃, R₁=CH₃, R₂=R_(5b)=Cl,R₃=R₄=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-5005-II-5282.

Table 146: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=R_(5b)=Cl,R₃=R₄=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-5283-II-5560.

Table 147: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-5561-II-5838.

Table 148: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-5839-II-6116.

Table 149: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-6117-II-6394.

Table 150: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-6395-II-6672.

Table 151: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-6673-II-6950.

Table 152: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-6951-II-7228.

Table 153: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-7229-II-7506.

Table 154: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-7507-II-7784.

Table 155: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-7785-II-8062.

Table 156: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-8063-II-8340.

Table 157: in general formula II-A, W=CH₃, R₁=CH₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-8341-II-8618.

Table 158: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-8619-II-8896.

Table 159: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=R₄=R_(5b)=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-8897-II-9174.

Table 160: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=R₄=R_(5b)=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-9175-II-9452.

Table 161: in general formula II-A, W=H, R₁=CHF₂, R₂=R_(5b)=Cl, R₃=R₄=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-9453-II-9730.

Table 162: in general formula II-A, W=H, R₁=CF₃, R₂=R_(5b)=Cl, R₃=R₄=H,the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those inTable 127 and corresponding to II-1-II-278 in table 127 in turn, therepresentative compounds are coded as II-9731-II-10008.

Table 163: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-10009-II-10286.

Table 164: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-10287-II-10564.

Table 165: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-10565-II-10842.

Table 166: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-10843-II-11120.

Table 167: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-11121-II-11398.

Table 168: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-11399-II-11676.

Table 169: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-11677-II-11954.

Table 170: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-11955-II-12232.

Table 171: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-12233-II-12510.

Table 172: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-12511-II-12788.

Table 173: in general formula II-A, W=H, R₁=CHF₂, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-12789-II-13066.

Table 174: in general formula II-A, W=H, R₁=CF₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-13067-II-13344.

Table 175: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl,R₃=R₄=R_(5b)=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-13345-II-13622.

Table 176: in general formula II-A, W=CH₃, R₁=CF₃, R₂=Cl,R₃=R₄=R_(5b)=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-13623-II-13900.

Table 177: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=R_(5b)=Cl,R₃=R₄=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-13901-II-14178.

Table 178: in general formula II-A, W=CH₃, R₁=CF₃, R₂=R_(5b)=Cl,R₃=R₄=H, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-14179-II-14456.

Table 179: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-14457-II-14734.

Table 180: in general formula II-A, W=CH₃, R₁=CF₃, R₂=Cl, R₃=R₄=H,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-14735-II-15012.

Table 181: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-15013-II-15290.

Table 182: in general formula II-A, W=CH₃, R₁=CF₃, R₂=Cl, R₃=R₄=H,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-15291-II-15568.

Table 183: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-15569-II-15846.

Table 184: in general formula II-A, W=CH₃, R₁=CF₃, R₂=Cl, R₃=R_(5b)=H,R₄=CH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-15847-II-16124.

Table 185: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-16125-II-16402.

Table 186: in general formula II-A, W=CH₃, R₁=CF₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Cl, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-16403-II-16680.

Table 187: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-16681-II-16958.

Table 188: in general formula II-A, W=CH₃, R₁=CF₃, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=Br, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent withthose in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-16959-II-17236.

Table 189: in general formula II-A, W=CH₃, R₁=CHF₂, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-17237-II-17514.

Table 190: in general formula II-A, W=CH₃, R₁=C₂H₅, R₂=Cl, R₃=H, R₄=CH₃,R_(5b)=OCH₃, the substituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistentwith those in Table 127 and corresponding to II-1-II-278 in table 127 inturn, the representative compounds are coded as II-17515-II-17792.

In general formula II-B, R₁=CH₃, R₂=Cl, R₇=R₈=R₁₀=R₁₁=H, R₉=CF₃, thesubstituent R₁₂ refers to Table 191, the representative compounds arecoded as II-17793-II-17932.

TABLE 191 No. R₁₂ II-17793 S-i-C₃H₇ II-17794 OH II-17795 —C(═O)HII-17796 CBr₃ II-17797 CH₃ II-17798 C₂H₅ II-17799 n-C₃H₇ II-17800 i-C₃H₇II-17801 n-C₄H₉ II-17802 i-C₄H₉ II-17803 t-C₄H₉ II-17804 CI₃ II-17805CH₂Br II-17806 CHF₂ II-17807 CHBr₂ II-17808 CF₃ II-17809 CH₂Cl II-17810CHCl₂ II-17811 CCl₃ II-17812 CH₂F II-17813 OCH₃ II-17814 OC₂H₅ II-17815OCH(CH₃)₂ II-17816 OC(CH₃)₃ II-17817 OCF₃ II-17818 OCH₂CF₃ II-17819OCH₂F II-17820 OCHF₂ II-17821 SCH₃ II-17822 SC₂H₅ II-17823 SCH₂CH═CH₂II-17824 CH═CH₂ II-17825 CH₂CH═CH₂ II-17826 CH₂CH═CCl₂ II-17827 C≡CHII-17828 CH₂C≡CH II-17829 CH₂C≡C—I II-17830 CH₂OCH₃ II-17831 CH₂OCH₂CH₃II-17832 CH₂CH₂OCH₃ II-17833 CH₂CH₂OCH₂CH₃ II-17834 CH₂OCH₂Cl II-17835CH₂OCH₂CH₂Cl II-17836 CH₂CH₂OCH₂Cl II-17837 CH₂SCH₃ II-17838 CH₂SCH₂CH₃II-17839 CH₂CH₂SCH₃ II-17840 CH₂CH₂SCH₂CH₃ II-17841 CH₂SCH₂Cl II-17842CH₂SCH₂CH₂Cl II-17843 CH₂CH₂SCH₂Cl II-17844 SOCH₃ II-17845 SOC₂H₅II-17846 SOCF₃ II-17847 SOCH₂CF₃ II-17848 SO₂CH₃ II-17849 SO₂C₂H₅II-17850 SO₂CF₃ II-17851 SO₂CH₂CF₃ II-17852 SO₂NHCOCH₃ II-17853 SO₂NHCH₃II-17854 SO₂N(CH₃)₃ II-17855 CONHSO₂CH₃ II-17856 COCH₃ II-17857 COC₂H₅II-17858 CO—n-C₃H₇ II-17859 CO—i-C₃H₇ II-17860 CO—n-C₄H₉ II-17861CO—i-C₄H₉ II-17862 CO—t-C₄H₉ II-17863 COCF₃ II-17864 COCH₂Cl II-17865COOCH₃ II-17866 COOC₂H₅ II-17867 COO—n-C₃H₇ II-17868 COO—t-C₄H₉ II-17869COOCF₃ II-17870 COOCH₂CH₂Cl II-17871 COOCH₂CF₃ II-17872 CH₂COOCH₃II-17873 CH₂COOC₂H₅ II-17874 CH₂COCH₃ II-17875 CH₂COC₂H₅ II-17876CONHCH₃ II-17877 CONHC₂H₅ II-17878 CONH—t-C₄H₉ II-17879 CON(CH₃)₂II-17880 CON(C₂H₅)₂ II-17881 COOCH₂CH═CH₂ II-17882 COOCH₂C≡CH II-17883COOCH₂OCH₃ II-17884 COOCH₂CH₂OCH₃ II-17885 SNHCH₃ II-17886 SNHC₂H₅II-17887 SN(CH₃)₂ II-17888 SN(C₂H₅)₂ II-17889

II-17890

II-17891

II-17892

II-17893

II-17894

II-17895

II-17896

II-17897

II-17898

II-17899

II-17900

II-17901

II-17902

II-17903

II-17904

II-17905

II-17906

II-17907

II-17908

II-17909

II-17910

II-17911

II-17912

II-17913

II-17914

II-17915

II-17916

II-17917

II-17918

II-17919

II-17920

II-17921

II-17922

II-17923

II-17924

II-17925

II-17926

II-17927

II-17928

II-17929

II-17930

II-17931

II-17932

Table 192: in general formula II-B, R₁=C₂H₅, R₂=Cl, R₇=R₈=R₁₀=R₁₁=H,R₉=CF₃, the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-17933-II-18072.

Table 193: in general formula II-B, R₁=CH₃, R₂=R₉=Cl, R₇=R₈=R₁₀=R₁₁=H,the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18073-II-18212.

Table 194: in general formula II-B, R₁=C₂H₅, R₂=R₉=Cl, R₇=R₈=R₁₀=R₁=H,the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18213-II-18352.

Table 195: in general formula II-B, R₁=CH₃, R₂=R₇=R₉=Cl, R₈=R₁₀=R₁₁=H,the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18353-II-18492.

Table 196: in general formula II-B, R₁=C₂H₅, R₂=R₇=R₉=Cl, R₈=R₁₀=R₁₁=H,the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18493-II-18632.

Table 197: in general formula II-B, R₁=CH₃, R₂=R₇=R₁₁=Cl, R₈=R₁₀=H,R₉=NO₂, the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18633-II-18772.

Table 198: in general formula II-B, R₁=C₂H₅, R₂=R₇=R₁=Cl, R₈=R₁₀=H,R₉=NO₂, the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18773-II-18912.

Table 199: in general formula II-B, R₁=CHF₂, R₂=R₉=Cl, R₇=R₈=R₁₀=R₁₁=H,the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-18913-II-19052.

Table 200: in general formula II-B, R₁=CHF₂, R₂=Cl, R₇=R₈=R₁₀=R₁₁=H,R₉=CF₃, the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-19053-II-19192.

Table 201: in general formula II-B, R₁=CHF₂, R₂=R₇=R₉=Cl, R₈=R₁₀=R₁₁=H,the substituent R₁₂ are consistent with those in Table 191 andcorresponding to II-17793-II-17932 in table 191 in turn, therepresentative compounds are coded as II-19193-II-19332.

The salts of some compounds having a structure as represented by formulaII of the present invention are listed in Table 202, but without beingrestricted thereby.

TABLE 202 the salts of some compounds No. structure II-19333

II-19334

II-19335

II-19336

II-19337

II-19338

II-19339

II-19340

II-19341

II-19342

II-19343

II-19344

II-19345

II-19346

II-19347

II-19348

II-19349

II-19350

II-19351

II-19352

II-19353

II-19354

II-19355

II-19356

II-19357

II-19358

II-19359

II-19360

II-19361

II-19362

II-19363

II-19364

II-19365

II-19366

II-19367

II-19368

II-19369

II-19370

II-19371

II-19372

II-19373

II-19374

II-19375

II-19376

II-19377

II-19378

II-19379

II-19380

II-19381

II-19382

II-19383

II-19384

II-19385

II-19386

II-19387

II-19388

II-19389

II-19390

II-19391

II-19392

II-19393

II-19394

II-19395

II-19396

II-19397

II-19398

II-19399

II-19400

II-19401

II-19402

II-19403

II-19404

II-19405

II-19406

II-19407

II-19408

II-19409

II-19410

II-19411

II-19412

II-19413

II-19414

II-19415

II-19416

II-19417

II-19418

II-19419

II-19420

II-19421

II-19422

II-19423

II-19424

II-19425

II-19426

II-19427

II-19428

II-19429

II-19430

II-19431

II-19432

II-19433

II-19434

II-19435

II-19436

In the general formula III, part of preferred substituents of R₁, R₂, W,R₃ and R₄ are separately listed in table 203 to table 206, but withoutbeing restricted thereby. The definitions of other substituents aredefined as above.

TABLE 203 R₁ substituents R₁ H F Cl Br I CH₃ C₂H₅ n-C₃H₇ i-C₃H₇ n-C₄H₉i-C₄H₉ t-C₄H₉

CH₂Cl CHCl₂ CH₂CH═CH₂ CCl₃ CHF₂ CHBr₂ CF₃ CH(CH₃)F CH(CH₃)Cl CH(CH₃)BrC(CH₃)₂F OCH₃ OC₂H₅ OCF₃ OCH₂CH═CH₂ OCH₂CH═CHCl OCH₂C≡CH OCH₂C≡C—IOCH₂C≡CCH₃ OSO₂CH₃ CH₂C≡CH SCH₃ SOCH₃ SO₂CH₃ COOH COOCH₃ COOC₂H₅ CONH₂CONHCH₃ CONHCN CONHCH₂CN CON(CH₃)₂ NH₂ NHCH₃ NHC₂H₅ N(CH₃)₂ N(C₂H₅)₂NHCH₂CN CH₂OCH₂Cl NHOCH₃ NHOC₂H₅ NHCOCH₃ NHCOC₂H₅ NHCOOCH₃ NHCOOC₂H₅N(CH₃)NH₂ NHN(CH₃)₂ CH₂OCH₃ CH₂OCH₂CH₃ CH₂CH₂OCH₃ CH₂CH₂OCH₂CH₃CH(CH₃)SCH₃ CH(CH₃)SOCH₃ CH(CH₃)SO₂CH₃ CH(CH₃)OH CH(CH₃)OCOCH₃CH₂OCH₂CH₂Cl

TABLE 204 R₂ substituents R₂ R₂ R₂ R₂ H NO₂ t-C₄H₉ OC₄H₉-i F CH₃ OCH₃OC₄H₉-t Cl C₂H₅ OC₂H₅ OCH₂F Br n-C₃H₇ OC₃H₇-n OCHF₂ I i-C₃H₇ OC₃H₇-iOCF₃ CN n-C₄H₉ OC₄H₉-n OCH₂CF₃

TABLE 205 W substituents W H F Cl Br I CH₃ C₂H₅ n-C₃H₇ i-C₃H₇ n-C₄H₉t-C₄H₉

CHCl₂ CCl₃ CHF₂ CHBr₂ CF₃ CH(CH₃)F CH(CH₃)Cl CH(CH₃)Br CH(n-C₄H₉)FC(CH₃)₂F OCH₃ OC₂H₅ OC₃H₇-n OC₃H₇-i OC₄H₉-n OC₄H₉-i OC₄H₉-t OCF₃ OCH₂CF₃SCH₃ SC₂H₅ SC₃H₇-n SC₃H₇-i SC₄H₉-n SC₄H₉-i SC₄H₉-t

TABLE 206 R₃(R₄)substituents R₃(R₄) H CH₃ C₂H₅ n-C₃H₇ i-C₃H₇ n-C₄H₉i-C₄H₉

t-C₄H₉ CH═CH₂ C≡CH CH₂CH═CH₂ CH₂C≡CH CH₂CH═CCl₂ CH₂C≡C—I CH₂OCH₃CH₂OCH₂CH₃ CH₂CH₂OCH₃ CH₂CH₂OCH₂CH₃

CR₃R₄

The present invention is also explained by the following compoundshaving a structure as represented by formula III listed in Table 207 toTable 304, but without being restricted thereby. The compounds having astructure as represented by formula III-A, III-B, III-C, III-D, III-E,III-F, III-G and III-H refer to Table 207 to Table 304, R_(5a)=R_(5c)=H.

In general formula III-A,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇, R₈, R₉, R₁₀and R₁₁ refer to Table 207, the representative compounds are coded asIII-1-III-180.

TABLE 207 No. R₇ R₈ R₉ R₁₀ R₁₁ III-1 H H H H H III-2 F H H H H III-3 H FH H H III-4 H H F H H III-5 Cl H H H H III-6 H Cl H H H III-7 H H Cl H HIII-8 Br H H H H III-9 H Br H H H III-10 H H Br H H III-11 I H H H HIII-12 H I H H H III-13 H H I H H III-14 CH₃ H H H H III-15 H CH₃ H H HIII-16 H H CH₃ H H III-17 OCH₃ H H H H III-18 H OCH₃ H H H III-19 H HOCH₃ H H III-20 CF₃ H H H H III-21 H CF₃ H H H III-22 H H CF₃ H H III-23OCF₃ H H H H III-24 H OCF₃ H H H III-25 H H OCF₃ H H III-26 NO₂ H H H HIII-27 H NO₂ H H H III-28 H H NO₂ H H III-29 CN H H H H III-30 H CN H HH III-31 H H CN H H III-32 CH(CH₃)₂ H H H H III-33 H CH(CH₃)₂ H H HIII-34 H H CH(CH₃)₂ H H III-35 H H t-Bu H H III-36 SCH₃ H H H H III-37 HSCH₃ H H H III-38 H H SCH₃ H H III-39 SCF₃ H H H H III-40 H SCF₃ H H HIII-41 H H SCF₃ H H III-42 COCH₃ H H H H III-43 H COCH₃ H H H III-44 H HCOCH₃ H H III-45 SOCH₃ H H H H III-46 H SOCH₃ H H H III-47 H H SOCH₃ H HIII-48 SO₂CH₃ H H H H III-49 H SO₂CH₃ H H H III-50 H H SO₂CH₃ H H III-51OCHF₂ H H H H III-52 H OCHF₂ H H H III-53 H H OCHF₂ H H III-54 CO₂CH₃ HH H H III-55 H CO₂CH₃ H H H III-56 H H CO₂CH₃ H H III-57 N(CH₃)₂ H H H HIII-58 H N(CH₃)₂ H H H III-59 H H N(CH₃)₂ H H III-60 N(C₂H₅)₂ H H H HIII-61 H N(C₂H₅)₂ H H H III-62 H H N(C₂H₅)₂ H H III-63 NHCOCH₃ H H H HIII-64 H NHCOCH₃ H H H III-65 H H NHCOCH₃ H H III-66 NHSO₂CH₃ H H H HIII-67 H NHSO₂CH₃ H H H III-68 H H NHSO₂CH₃ H H III-69 OCH₂CH═CH₂ H H HH III-70 H OCH₂CH═CH₂ H H H III-71 H H OCH₂CH═CH₂ H H III-72 OCH₂C≡CH HH H H III-73 H OCH₂C≡CH H H H III-74 H H OCH₂C≡CH H H III-75 F F H H HIII-76 F H F H H III-77 F H H F H III-78 F H H H F III-79 H F F H HIII-80 H F H F H III-81 Cl Cl H H H III-82 Cl H Cl H H III-83 Cl H H ClH III-84 Cl H H H Cl III-85 H Cl Cl H H III-86 H Cl H Cl H III-87 NO₂ HNO₂ H H III-88 NO₂ H H NO₂ H III-89 NO₂ H H H NO₂ III-90 H NO₂ H NO₂ HIII-91 CN H CN H H III-92 CN H H CN H III-93 CN H H H CN III-94 H CN HCN H III-95 CH₃ CH₃ H H H III-96 CH₃ H CH₃ H H III-97 CH₃ H H CH₃ HIII-98 CH₃ H H H CH₃ III-99 H CH₃ CH₃ H H III-100 H CH₃ H CH₃ H III-101CF₃ H CF₃ H H III-102 CF₃ H H CF₃ H III-103 CF₃ H H H CF₃ III-104 H CF₃H CF₃ H III-105 OCF₃ H OCF₃ H H III-106 OCF₃ H H OCF₃ H III-107 OCF₃ H HH OCF₃ III-108 H OCF₃ H OCF₃ H III-109 CH₃ Cl H H H III-110 CH₃ H Cl H HIII-111 H Cl CH₃ H H III-112 Cl H CH₃ H H III-113 CH₃ H H Cl H III-114CH₃ H H H Cl III-115 Br CH₃ H H H III-116 H CH₃ Cl H H III-117 CH₃ NO₂ HH H III-118 CH₃ H NO₂ H H III-119 CH₃ H OCH₃ H H III-120 CH₃ H H NO₂ HIII-121 Cl H CF₃ H H III-122 Cl H H CF₃ H III-123 Cl H NO₂ H H III-124Cl H H NO₂ H III-125 CF₃ H Br H H III-126 CF₃ H NO₂ H H III-127 H CF₃NO₂ H H III-128 H CF₃ Cl H H III-129 CF₃ H CN H H III-130 Cl H CN H HIII-131 NO₂ H CN H H III-132 NO₂ H CH₃ H H III-133 NO₂ H CF₃ H H III-134NO₂ H Cl H H III-135 NO₂ H H Cl H III-136 H NO₂ CH₃ H H III-137 H NO₂ ClH H III-138 CN F H H H III-139 CN H NO₂ H H III-140 CN H Cl H H III-141CN H H CH₃ H III-142 Cl Cl Cl H H III-143 Cl Cl H Cl H III-144 Cl H ClCl H III-145 Cl H Cl H Cl III-146 H Cl Cl Cl H III-147 CH₃ H CH₃ H CH₃III-148 OCH₃ H OCH₃ H OCH₃ III-149 Cl Cl Br H H III-150 F H F H ClIII-151 CH₃ H Br H Br III-152 CF₃ H Cl H Cl III-153 CF₃ H Br H BrIII-154 F H Cl H Br III-155 Cl H NO₂ H Cl III-156 Br H NO₂ H Br III-157Cl H CN H Cl III-158 Cl H CF₃ H Cl III-159 Br H CF₃ H Br III-160 Cl CH₃H H Cl III-161 Cl H CONH₂ H Cl III-162 Cl H CO₂CH₃ H Cl III-163 Cl HNHCOCH₃ H Cl III-164 Cl H OCF₃ H Cl III-165 Br H F H Br III-166 Br H CH₃H Br III-167 Cl H COCH₃ H Cl III-168 Cl H NO₂ Cl H III-169 F H F H ClIII-170 Cl H CF₃ H Br III-171 CH₃ H NO₂ H Cl III-172 CH₃ H NO₂ H BrIII-173 CH₃ H Cl H NO₂ III-174 CH₃ H Br H NO₂ III-175 NO₂ H CF₃ H ClIII-176 NO₂ H CF₃ H Br III-177 F H Br H Br III-178 CN H Cl H Cl III-179CN H Br H Br III-180 F H CN H H

Table 208: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-181-III-360.

Table 209: A=NH, R₁=CF₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the s substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-361-III-540.

Table 210: A=NH, R₁=CHF₂, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-541-III-720.

Table 211: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-721-III-900.

Table 212: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-901-III-1080.

Table 213: A=NH, R₁=CF₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-1081-III-1260.

Table 214: A=NH, R₁=CHF₂, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-1261-III-1440.

Table 215: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-1441-III-1620.

Table 216: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-1621-III-1800.

Table 217: A=NH, R₁=CF₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-1801-III-1980.

Table 218: A=NH, R₁=CHF₂, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-1981-III-2160.

Table 219: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=H, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-2161-III-2340.

Table 220: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=H, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-2341-III-2520.

Table 221: A=NH, R₁=Cl, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-2521-III-2700.

Table 222: A=NH, R₁=CHF₂, R₂=Cl, W=CH₃, R₃=R₄=H, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-2701-III-2880.

Table 223: A=NH, R₁=CH₃, R₂=Cl, W=R₄=R_(5b)=H, R₃=CH₃, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-2881-III-3060.

Table 224: A=NH, R₁=C₂H₅, R₂=Cl, W=R₄=R_(5b)=H, R₃=CH₃, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-3061-III-3240.

Table 225: A=NH, R₁=CH₃, R₂=Cl, W=R₄=H, R₃=CH₃, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-3241-III-3420.

Table 226: A=NH, R₁=C₂H₅, R₂=Cl, W=R₄=H, R₃=CH₃, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-3421-III-3600.

Table 227: A=NH, R₁=CH₃, R₂=Cl, W=R_(5b)=H, R₃=R₄=CH₃, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-3601-III-3780.

Table 228: A=NH, R₁=C₂H₅, R₂=Cl, W=R_(5b)=H, R₃=R₄=CH₃, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-3781-III-3960.

Table 229: A=NH, R₁=CH₃, R₂=Cl, W=H, R₃=R₄=CH₃, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-3961-III-4140.

Table 230: A=NH, R₁=C₂H₅, R₂=Cl, W=H, R₃=R₄=CH₃, R_(5b)=Cl, thesubstituents R₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table207 and corresponding to III-1-III-180 in table 207 in turn, therepresentative compounds are coded as III-4141-III-4320.

Table 231: A=O, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-4321-III-4500.

Table 232: A=O, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-4501-III-4680.

Table 233: A=O, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-4681-III-4860.

Table 234: A=O, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-4861-III-5040.

Table 235: A=S, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-5041-III-5220.

Table 236: A=S, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-5221-III-5400.

Table 237: A=S, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-5401-III-5580.

Table 238: A=S, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 207 andcorresponding to III-1-III-180 in table 207 in turn, the representativecompounds are coded as III-5581-III-5760.

In general formula III-B,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈, R₉, R₁₀ andR₁₁ refer to Table 239, the representative compounds are coded asIII-5761-III-5802.

TABLE 239 No. R₈ R₉ R₁₀ R₁₁ III-5761 H H H H III-5762 H H H F III-5763 HH H Cl III-5764 H H H Br III-5765 H H Cl H III-5766 H Cl H H III-5767 HBr H H III-5768 Cl H H H III-5769 H H H NO₂ III-5770 H H NO₂ H III-5771H NO₂ H H III-5772 H CN H H III-5773 H OCF₃ H H III-5774 H H H CH₃III-5775 H H CH₃ H III-5776 H CH₃ H H III-5777 CH₃ H H H III-5778 H H HCF₃ III-5779 H H CF₃ H III-5780 H CF₃ H H III-5781 H H H OCH₃ III-5782 HH OCH₃ H III-5783 H OCH₃ H H III-5784 OCH₃ H H H III-5785 H Cl H ClIII-5786 Cl H Cl H III-5787 H NO₂ H Cl III-5788 H CN H Cl III-5789 H CF₃H Cl III-5790 H NO₂ H Br III-5791 H H Cl NO₂ III-5792 H Cl H NO₂III-5793 H CN H CH₃ III-5794 H Br CH₃ H III-5795 H NO₂ CH₃ H III-5796CH₃ H CH₃ H III-5797 H Cl H CF₃ III-5798 Cl H H CF₃ III-5799 CH₃ Cl CH₃Cl III-5800 Cl Cl H Cl III-5801 Cl CF₃ H Br III-5802 H Br CH₃ Br

Table 240: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 239 and correspondingto III-5761-III-5802 in table 239 in turn, the representative compoundsare coded as III-5803-III-5844.

Table 241: A=NH, R₁=CF₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 239 and correspondingto III-5761-III-5802 in table 239 in turn, the representative compoundsare coded as III-5845-III-5886.

Table 242: A=NH, R₁=CHF₂, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 239 and correspondingto III-5761-III-5802 in table 239 in turn, the representative compoundsare coded as III-5887-III-5928.

Table 243: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 239 andcorresponding to III-5761-III-5802 in table 239 in turn, therepresentative compounds are coded as III-5929-III-5970.

Table 244: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 239 andcorresponding to III-5761-III-5802 in table 239 in turn, therepresentative compounds are coded as III-5971-III-6012.

Table 245: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 239 andcorresponding to III-5761-III-5802 in table 239 in turn, therepresentative compounds are coded as III-6013-III-6054.

Table 246: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 239 andcorresponding to III-5761-III-5802 in table 239 in turn, therepresentative compounds are coded as III-6055-III-6096.

Table 247: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 239 andcorresponding to III-5761-III-5802 in table 239 in turn, therepresentative compounds are coded as III-6097-III-6138.

Table 248: A=O, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 239 and correspondingto III-5761-III-5802 in table 239 in turn, the representative compoundsare coded as III-6139-III-6180.

Table 249: A=S, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 239 and correspondingto III-5761-III-5802 in table 239 in turn, the representative compoundsare coded as III-6181-III-6222.

Table 250: A=S, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 239 and correspondingto III-5761-III-5802 in table 239 in turn, the representative compoundsare coded as III-6223-III-6264.

In general formula III-C,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇, R₉, R₁₀ andR₁₁ refer to Table 251, the representative compounds are coded asIII-6265-III-6282.

TABLE 251 No. R₇ R₉ R₁₀ R₁₁ III-6265 H H H H III-6266 Cl H H H III-6267OCH₃ H H H III-6268 OCH₂CF₃ H H H III-6269 H H H CH₃ III-6270 H H H CF₃III-6271 H Br H H III-6272 H CF₃ H H III-6273 H OCH₃ H H III-6274 Cl HCl H III-6275 Cl Cl H H III-6276 H Cl Cl H III-6277 Cl H H CH₃ III-6278Cl H CH₃ H III-6279 Cl CH₃ H H III-6280 Cl Cl H CF₃ III-6281 H NHCH₃ ClH III-6282 H SO₂CH₃ Cl H

Table 252: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₉, R₁₀ and R₁₁ are consistent with those in Table 251 and correspondingto III-6265-III-6282 in table 251 in turn, the representative compoundsare coded as III-6283-III-6300.

Table 253: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₉, R₁₀ and R₁₁ are consistent with those in Table 251 andcorresponding to III-6265-III-6282 in table 251 in turn, therepresentative compounds are coded as III-6301-III-6318.

Table 254: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₉, R₁₀ and R₁₁ are consistent with those in Table 251 andcorresponding to III-6265-III-6282 in table 251 in turn, therepresentative compounds are coded as III-6319-III-6336.

Table 255: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₉, R₁₀ and R₁₁ are consistent with those in Table 251 andcorresponding to III-6265-III-6282 in table 251 in turn, therepresentative compounds are coded as III-6337-III-6354.

Table 256: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₉, R₁₀ and R₁₁ are consistent with those in Table 251 andcorresponding to III-6265-III-6282 in table 251 in turn, therepresentative compounds are coded as III-6355-III-6372.

In general formula III-D,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇, R₈, R₁₀ andR₁₁ refer to Table 257, the representative compounds are coded asIII-6373-III-6380.

TABLE 257 No. R₇ R₈ R₁₀ R₁₁ III-6373 H H Cl H III-6374 H H H Br III-6375Cl H H Cl III-6376 H H OCH₃ H III-6377 H OCH₃ OCH₃ H III-6378 H Cl OCH₃H III-6379 H Cl NHCH₃ H III-6380 Cl Cl Cl Cl

Table 258: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₈, R₁₀ and R₁₁ are consistent with those in Table 257 and correspondingto III-6373-III-6380 in table 257 in turn, the representative compoundsare coded as III-6381-III-6388.

Table 259: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₁₀ and R₁₁ are consistent with those in Table 257 andcorresponding to III-6373-III-6380 in table 257 in turn, therepresentative compounds are coded as III-6389-III-6396.

Table 260: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₈, R₁₀ and R₁₁ are consistent with those in Table 257 andcorresponding to III-6373-III-6380 in table 257 in turn, therepresentative compounds are coded as III-6397-III-6404.

Table 261: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₁₀ and R₁₁ are consistent with those in Table 257 andcorresponding to III-6373-III-6380 in table 257 in turn, therepresentative compounds are coded as III-6405-III-6412.

Table 262: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₈, R₁₀ and R₁₁ are consistent with those in Table 257 andcorresponding to III-6373-III-6380 in table 257 in turn, therepresentative compounds are coded as III-6413-III-6420.

In general formula III-E,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈, R₉, R₁₀ andR₁₁ refer to Table 263, the representative compounds are coded asIII-6421-III-6424.

TABLE 263 No. R₈ R₉ R₁₀ III-6421 H H H III-6422 CH₃ H CH₃ III-6423 OCH₃H OCH₃ III-6424 CO₂C₂H₅ H CF₃

Table 264: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₉, R₁₀ and R₁₁ are consistent with those in Table 263 and correspondingto III-6421-III-6424 in table 263 in turn, the representative compoundsare coded as III-6425-III-6428.

Table 265: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 263 andcorresponding to III-6421-III-6424 in table 263 in turn, therepresentative compounds are coded as III-6429-III-6432.

Table 266: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 263 andcorresponding to III-6421-III-6424 in table 263 in turn, therepresentative compounds are coded as III-6433-III-6436.

Table 267: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 263 andcorresponding to III-6421-III-6424 in table 263 in turn, therepresentative compounds are coded as III-6437-III-6440.

Table 268: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₉, R₁₀ and R₁₁ are consistent with those in Table 263 andcorresponding to III-6421-III-6424 in table 263 in turn, therepresentative compounds are coded as III-6441-III-6444.

In general formula III-F,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈, R₁₀ and Rrefer to Table 269, the representative compounds are coded asIII-6445-III-6448.

TABLE 269 No. R₈ R₁₀ R₁₁ III-6445 H H H III-6446 H Cl H III-6447 CH₃ ClH III-6448 H Cl Cl

Table 270: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₈,R₁₀ and R₁₁ are consistent with those in Table 269 and corresponding toIII-6445-III-6448 in table 269 in turn, the representative compounds arecoded as III-6449-III-6452.

Table 271: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₈, R₁₀ and R₁₁ are consistent with those in Table 269 and correspondingto III-6445-III-6448 in table 269 in turn, the representative compoundsare coded as III-6453-III-6456.

Table 272: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₈, R₁₀ and R₁₁ are consistent with those in Table 269 and correspondingto III-6445-III-6448 in table 269 in turn, the representative compoundsare coded as III-6457-III-6460.

Table 273: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₁₀ and R₁₁ are consistent with those in Table 269 and correspondingto III-6445-III-6448 in table 269 in turn, the representative compoundsare coded as III-6461-III-6464.

Table 274: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₈, R₁₀ and R₁₁ are consistent with those in Table 269 and correspondingto III-6445-III-6448 in table 269 in turn, the representative compoundsare coded as III-6465-III-6468.

In general formula III-G,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇, R₉ and R₁₀refer to Table 275, the representative compounds are coded asIII-6469-III-6470.

TABLE 275 No. R₇ R₉ R₁₀ III-6469 H H H III-6470 H H Cl

Table 276: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₇,R₉ and R₁₀ are consistent with those in Table 275 and corresponding toIII-6469-III-6470 in table 275 in turn, the representative compounds arecoded as III-6471-III-6472.

Table 277: A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₉ and R₁₀ are consistent with those in Table 275 and correspondingto III-6469-III-6470 in table 275 in turn, the representative compoundsare coded as III-6473-III-6474.

Table 278: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₇, R₉ and R₁₀ are consistent with those in Table 275 and correspondingto III-6469-III-6470 in table 275 in turn, the representative compoundsare coded as III-6475-III-6476.

Table 279: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₉ and R₁₀ are consistent with those in Table 275 and correspondingto III-6469-III-6470 in table 275 in turn, the representative compoundsare coded as III-6477-III-6478.

Table 280: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₇, R₉ and R₁₀ are consistent with those in Table 275 and correspondingto III-6469-III-6470 in table 275 in turn, the representative compoundsare coded as III-6479-III-6480.

In general formula III-H,

A=NH, R₁=CH₃, R₂=Cl, W=R₃=R₄=R_(5b)=H, the substituents R₉, R₁₀ and Rrefer to Table 281, the representative compounds are coded asIII-6481-III-6482.

TABLE 281 No. R₉ R₁₀ R₁₁ III-6481 H H H III-6482 Cl H H

Table 284: A=NH, R₁=C₂H₅, R₂=Cl, W=R₃=R₄=H, R_(5b)=Cl, the substituentsR₉, R₁₀ and R₁₁ are consistent with those in Table 281 and correspondingto III-6481-III-6482 in table 281 in turn, the representative compoundsare coded as III-6487-III-6488.

Table 285: A=NH, R₁=CH₃, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₉, R₁₀ and R₁₁ are consistent with those in Table 281 and correspondingto III-6481-III-6482 in table 281 in turn, the representative compoundsare coded as III-6489-III-6490

Table 286: A=NH, R₁=C₂H₅, R₂=Cl, W=CH₃, R₃=R₄=R_(5b)=H, the substituentsR₉, R₁₀ and R₁₁ are consistent with those in Table 281 and correspondingto III-6481-III-6482 in table 281 in turn, the representative compoundsare coded as III-6491-III-6492.

In general formula III-A, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₇=R₈=R₁₀=R₁₁=H, R₉=Cl, the substituents R₁₂ refer toTable 287, the representative compounds are coded as III-6493-III-6632.

TABLE 287 No. R₁₂ III-6493 S—i-C₃H₇ III-6494 OH III-6495 —C(═O)HIII-6496 CBr₃ III-6497 CH₃ III-6498 C₂H₅ III-6499 n-C₃H₇ III-6500 i-C₃H₇III-6501 n-C₄H₉ III-6502 i-C₄H₉ III-6503 t-C₄H₉ III-6504 CI₃ III-6505CH₂Br III-6506 CHF₂ III-6507 CHBr₂ III-6508 CF3 III-6509 CH₂Cl III-6510CHCl₂ III-6511 CCl₃ III-6512 CH₂F III-6513 OCH₃ III-6514 OC₂H₅ III-6515OCH(CH₃)₂ III-6516 OC(CH₃)₃ III-6517 OCF₃ III-6518 OCH₂CF₃ III-6519OCH₂F III-6520 OCHF₂ III-6521 SCH₃ III-6522 SC₂H₅ III-6523 SCH₂CH═CH₂III-6524 CH═CH₂ III-6525 CH₂CH═CH₂ III-6526 CH₂CH═CCl₂ III-6527 C≡CHIII-6528 CH₂C≡CH III-6529 CH₂C≡C—I III-6530 CH₂OCH₃ III-6531 CH₂OCH₂CH₃III-6532 CH₂CH₂OCH₃ III-6533 CH₂CH₂OCH₂CH₃ III-6534 CH₂OCH₂Cl III-6535CH₂OCH₂CH₂Cl III-6536 CH₂CH₂OCH₂Cl III-6537 CH₂SCH₃ III-6538 CH₂SCH₂CH₃III-6539 CH₂CH₂SCH₃ III-6540 CH₂CH₂SCH₂CH₃ III-6541 CH₂SCH₂Cl III-6542CH₂SCH₂CH₂Cl III-6543 CH₂CH₂SCH₂Cl III-6544 SOCH₃ III-6545 SOC₂H₅III-6546 SOCF₃ III-6547 SOCH₂CF₃ III-6548 SO₂CH₃ III-6549 SO₂C₂H₅III-6550 SO₂CF₃ III-6551 SO₂CH₂CF₃ III-6552 SO₂NHCOCH₃ III-6553 SO₂NHCH₃III-6554 SO₂N(CH₃)₃ III-6555 CONHSO₂CH₃ III-6556 COCH₃ III-6557 COC₂H₅III-6558 CO—n-C₃H₇ III-6559 CO—i-C₃H₇ III-6560 CO—n-C₄H₉ III-6561CO—i-C₄H₉ III-6562 CO—t-C₄H₉ III-6563 COCF₃ III-6564 COCH₂Cl III-6565COOCH₃ III-6566 COOC₂H₅ III-6567 COO—n-C₃H₇ III-6568 COO—t-C₄H₉ III-6569COOCF₃ III-6570 COOCH₂CH₂Cl III-6571 COOCH₂CF₃ III-6572 CH₂COOCH₃III-6573 CH₂COOC₂H₅ III-6574 CH₂COCH₃ III-6575 CH₂COC₂H₅ III-6576CONHCH₃ III-6577 CONHC₂H₅ III-6578 CONH—t-C₄H₉ III-6579 CON(CH₃)₂III-6580 CON(C₂H₅)₂ III-6581 COOCH₂CH═CH₂ III-6582 COOCH₂C≡CH III-6583COOCH₂OCH₃ III-6584 COOCH₂CH₂OCH₃ III-6585 SNHCH₃ III-6586 SNHC₂H₅III-6587 SN(CH₃)₂ III-6588 SN(C₂H₅)₂ III-6589

III-6590

III-6591

III-6592

III-6593

III-6594

III-6595

III-6596

III-6597

III-6598

III-6599

III-6600

III-6601

III-6602

III-6603

III-6604

III-6605

III-6606

III-6607

III-6608

III-6609

III-6610

III-6611

III-6612

III-6613

III-6614

III-6615

III-6616

III-6617

III-6618

III-6619

III-6620

III-6621

III-6622

III-6623

III-6624

III-6625

III-6626

III-6627

III-6628

III-6629

III-6630

III-6631

III-6632

Table 288: in general formula III-A, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, R₇=R₉=Cl, the substituent R₁₂ areconsistent with those in Table 287 and corresponding toIII-6493-III-6632 in table 287 in turn, the representative compounds arecoded as III-6633-III-6772.

Table 289: in general formula Ill-A, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₇=R₈==R₁₀=R₁₁=H, R₉=CF₃, the substituent R₁₂ areconsistent with those in Table 287 and corresponding toIII-6493-III-6632 in table 287 in turn, the representative compounds arecoded as III-6773-III-6912.

Table 290: in general formula III-B, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, R₉=Cl, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-6913-III-7052.

Table 291: in general formula III-B, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₈=R₁₀=R₁₁=H, R₉=CF₃, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-7053-III-7192.

Table 292: in general formula III-B, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₈=R₁₀=H, R₉=CF₃, R₁₁=Cl, the substituent R₁₂ areconsistent with those in Table 287 and corresponding toIII-6493-III-6632 in table 287 in turn, the representative compounds arecoded as III-7193-III-7332.

Table 293: in general formula III-B, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₈=R₁₀=H, R₉=R₁₁=Cl, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-7333-III-7472.

Table 294: in general formula III-C, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₉=R₁₀=R₁₁=H, R₇=Cl, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-7473-III-7612.

Table 295: in general formula III-D, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₇=R₁₁=H, R₈=R₁₀=Cl, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-7613-III-7752.

Table 296: in general formula III-E, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₉=H, R₈=R₁₀=OCH₃, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-7753-III-7892.

Table 297: in general formula III-E, A=NR₁₂, R₁=C₂H₅, R₂=Cl,W=R₃=R₄=R_(5b)=R₉=H, R₈=R₁₀=CH₃, the substituent R₁₂ are consistent withthose in Table 287 and corresponding to III-6493-III-6632 in table 287in turn, the representative compounds are coded as III-7893-III-8032.

Table 298: in general formula III-F, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₈=H, R₁₀=CH₃, R₁₁=Cl, the substituent R₁₂ are consistentwith those in Table 287 and corresponding to III-6493-III-6632 in table287 in turn, the representative compounds are coded asIII-8033-III-8172.

Table 299: in general formula III-G, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₇=R₉=H, R₁₀=Cl, the substituent R₁₂ are consistent withthose in Table 287 and corresponding to III-6493-III-6632 in table 287in turn, the representative compounds are coded as III-8173-III-83122.

Table 300: in general formula Ill-H, A=NR₁₂, R₁=CH₃, R₂=Cl,W=R₃=R₄=R_(5b)=R₁₀=R₁₁=H, R₇=Cl, the substituent R₁₂ are consistent withthose in Table 287 and corresponding to III-6493-III-6632 in table 287in turn, the representative compounds are coded as III-8313-III-8452.

The salts of some compounds having a structure as represented by formulaIII of the present invention are listed in Table 301, but without beingrestricted thereby.

TABLE 301 the salts of some compounds No. structure III-8453

III-8454

III-8455

III-8456

III-8457

III-8458

III-8459

III-8460

III-8461

III-8462

III-8463

III-8464

III-8465

III-8466

III-8467

III-8468

III-8469

III-8470

III-8471

III-8472

III-8473

III-8474

III-8475

III-8476

III-8477

III-8478

III-8479

III-8480

III-8481

III-8482

III-8483

III-8484

III-8485

III-8486

III-8487

III-8488

III-8489

III-8490

III-8491

III-8492

III-8493

III-8494

III-8495

III-8496

The compounds represented by general formula PY of the invention can beprepared according to three schemes in which Substituent A can bedefined as different substituents, the definitions of each substituentis defined as above:

Scheme 1 to prepare the compounds represented by general formula PY:when A=NH, the compounds represented by general formula PY-1 can beprepared according to the following two schemes.

Method 1: the compounds represented by general formula PY-1 can beprepared by reaction of intermediates i and ii in the presence of properbase, the preparation methods are shown as follows.

The reaction was carried out in proper solvent and the proper solventmentioned may be selected from benzene, toluene, xylene, acetone,butanone, methylisobutylketone, tetrahydrofuran, acetonitrile,1,4-dioxane, DMF, N-methyl pyrrolidone, DMSO, pyridine, dichloromethane,chloroform, dichloroethane, methyl acetate or ethyl acetate and so on.

The reaction above can be carried out in the presence or absence ofbase, the reaction is promoted in the presence of base. Proper basementioned may be selected from alkali metal hydride such as sodiumhydride; alkali metal hydroxides such as sodium hydroxide or potassiumhydroxide; alkali metal carbonate such as sodium carbonate or potassiumcarbonate; organic amine such as pyridine or triethylamine.

The proper temperature mentioned is from room temperature to boilingpoint of the solvent, normal temperature is from 20 to 100° C.

The reaction time is in the range of 30 minutes to 20 hours, generallybeing 1-10 hours.

The detailed operation refers to the methods described in EP0370704,EP0356158, EP0264217, EP0665225, JP10036355 or U.S. Pat. No. 4,985,426.

Intermediates I are commercially available, or prepared according to themethods described in JP2000007662, U.S. Pat. No. 4,977,264, U.S. Pat.No. 6,090,815, US20040092402, JP09124613, U.S. Pat. No. 5,468,751, U.S.Pat. No. 4,985,426, U.S. Pat. No. 4,845,097, Recueil des TravauxChimiques des Pays-Bas (1978), 97(11), Pages 288-92, Journal of theAmerican Chemical Society, 79, 1455(1957) or Journal of ChemicalSociety, p. 3478-3481 (1955).

Intermediates ii are commercially available, or prepared according tothe methods described in U.S. Pat. No. 4,895,849, JP10036355, EP665225,US20070093498, WO2007046809, U.S. Pat. No. 5,783,522A, WO02083647A1,CN1927860A, WO9404527, US20110054173, WO2011025505, WO2004093800A, WO2012075917, US20050648509, US2002082454, Organic Syntheses, Coll. Vol.10, p. 501 (2004); Vol. 75, p. 61 (1998) or Organic Syntheses, Coll.Vol. 10, p. 102 (2004); Vol. 75, p. 53 (1998).

Method 2: the compounds represented by general formula iv can beprepared by reaction of intermediates i and iii in proper solvent, thenthe compounds represented by general formula PY-1 can be prepared byreaction of intermediates iv and v in the presence of proper base, thepreparation methods are shown as follows. Wherein, L is a leaving group,selected from halogen, boric acid, methyl methanesulfonate orp-toluenesulfonates.

The reaction was carried out between the intermediates represented bygeneral formula i and iii in proper solvent and the proper solventmentioned may be selected from benzene, toluene, xylene, acetone,butanone, methylisobutylketone, tetrahydrofuran, acetonitrile,1,4-dioxane, DMF, N-methyl pyrrolidone, DMSO, pyridine, dichloromethane,chloroform, dichloroethane, methyl acetate or ethyl acetate and so on.The reaction above can be carried out in the presence or absence ofbase, the reaction is promoted in the presence of base. Proper basementioned may be selected from alkali metal hydride such as sodiumhydride; alkali metal hydroxides such as sodium hydroxide or potassiumhydroxide; alkali metal carbonate such as sodium carbonate or potassiumcarbonate; organic amine such as pyridine or triethylamine.

The proper temperature mentioned is from room temperature to boilingpoint of the solvent, normal temperature is from 20 to 100° C. Thereaction time is in the range of 30 minutes to 20 hours, generally being1-10 hours.

The reaction was carried out between the intermediates represented bygeneral formula iv and v in proper solvent and the proper solventmentioned may be selected from benzene, toluene, xylene, acetone,butanone, methylisobutylketone, tetrahydrofuran, acetonitrile,1,4-dioxane, DMF, N-methyl pyrrolidone, DMSO, pyridine, dichloromethane,chloroform, dichloroethane, methyl acetate or ethyl acetate and so on.The reaction above can be carried out in the presence of base. Properbase mentioned may be selected from alkali metal hydride such as sodiumhydride; alkali metal hydroxides such as sodium hydroxide or potassiumhydroxide; alkali metal carbonate such as sodium carbonate or potassiumcarbonate; organic amine such as pyridine or triethylamine.

The proper temperature mentioned is from room temperature to boilingpoint of the solvent, normal temperature is from 20 to 200° C. Thereaction time is in the range of 30 minutes to 20 hours, generally being1-10 hours.

The detailed operation refers to the methods described in JP11049759,EP0370704, EPO 196524 or U.S. Pat. No. 4,895,849.

Other materials, such as the compounds represented by general formulaiii and v, used to prepare the compounds represented by general formulaPY-1, are commercially available.

The intermediate represented by general formula ii is one of keyintermediate, some compounds are commercially available, or are preparedaccording to the known method described above, also can be preparedaccording to the following two schemes in which Substituent X₁ can bedefined as different substituents.

Method 1: when X₁=CR₆, the intermediate ii used to prepare the compoundsrepresented by the general formula I and II (wherein A=NH) can beprepared according to the following two schemes. Relevant intermediatesare commercially available, or prepared according to the methodsdescribed in U.S. Pat. No. 4,895,849, JP10036355, EP665225,US20070093498, WO2007046809, U.S. Pat. No. 5,783,522A, WO02083647A1,CN1927860A, Organic Syntheses, Coll. Vol. 10, p. 501 (2004); Vol. 75, p.61 (1998) or Organic Syntheses, Coll. Vol. 10, p. 102 (2004); Vol. 75,p. 53 (1998).

(1) Reduction of Cyano:

Wherein, L is a leaving group, selected from halogen, boric acid, methylmethanesulfonate or p-toluenesulfonates. B is a alkyl chain with onemore carbon than M.

The compounds represented by general formula ii-c can be prepared byreaction of intermediates ii-a and ii-b in proper solvent in thepresence of proper base. The detailed operation refers to the methodsdescribed in US2002082454 and Fine Chemicals, 2005, 22(12): 944-960. Theproper temperature mentioned is from room temperature to boiling pointof the solvent, normal temperature is from 20 to 100° C. The reactiontime is in the range of 30 minutes to 20 hours, generally being 1-10hours. The proper solvent mentioned may be selected from acetone,butanone, tetrahydrofuran, acetonitrile, toluene, xylene, benzene, DMF,DMSO, methanol or ethanol and so on. Proper base mentioned may beselected from potassium hydroxide, sodium hydroxide, sodium carbonate,potassium carbonate, sodium bicarbonate, triethylamine, pyridine orsodium hydride.

When L refers to boric acid group, the compounds represented by generalformula ii-c can also be prepared by reaction of intermediates ii-a andii-b at 0-100° C. in proper solvent in the presence of proper base andcatalyst. The proper solvent mentioned may be selected from benzene,toluene, xylene, chloroform, dichloromethane, acetone, butanone,tetrahydrofuran, acetonitrile, 1,4-dioxane, DMF, N-methyl pyrrolidone orDMSO and so on. Proper base mentioned may be selected from pyridine ortriethylamine and so on. Proper catalyst mentioned may be selected fromcopper acetate, copper chloride or copper sulfate and so on.

The intermediates represented by general formula ii-1 can be prepared byreaction of intermediates represented by general formula ii-c andammonia water in the presence of proper catalyst by using hydrogenationreduction. The detailed operation refers to the methods described in J.Am. Chem. Soc, 70, 3788 (1948); 82, 681 (1960); 82, 2386 (1960); Can. J.Chem, 49, 2990 (1971); J. Org. Chem, 37, 335 (1972); Organic Syntheses,Coll. Vol. 3, p. 229, p. 720 (1955), Vol. 23, p. 71 (1943) or Vol. 27,p. 18 (1947). The proper temperature mentioned is from room temperatureto boiling point of the solvent, normal temperature is from 20 to 100°C. The reaction time is in the range of 30 minutes to 20 hours,generally being 1-10 hours. The proper solvent mentioned may be selectedfrom methanol, ethanol, isopropanol, benzene, toluene, xylene, acetone,butanone, methylisobutylketone, chloroform, dichloroethane, methylacetate, ethyl acetate, tetrahydrofuran, 1,4-dioxane, DMF, N-methylpyrrolidone or DMSO, etc. The proper catalysts mentioned may be selectedfrom Raney-nickel, palladium carbon or platinum oxide, etc.

(2) The method to prepare the substituted amine and its salts byreaction of the substituted 4-hydroxyphenylalkyl amine

Wherein, Boc₂O refers to di-tert-butyl dicarbonate.

Firstly, the compounds represented by general formula ii-e can beprepared by reaction of intermediates ii-d and di-tert-butyl dicarbonateat 0-100° C. in proper solvent in the presence of proper base. Thepreferred temperature is 0-50° C. The reaction time is in the range of30 minutes to 20 hours, generally being 0.5-10 hours. The proper solventmentioned may be selected from benzene, toluene, xylene, chloroform,dichloromethane, tetrahydrofuran, acetonitrile, 1,4-dioxane, DMF,N-methyl pyrrolidone or DMSO and so on. Proper base mentioned may beselected from alkali metal carbonate such as sodium carbonate, sodiumbicarbonate, potassium carbonate or potassium bicarbonate.

Then the compounds represented by general formula ii-f can be preparedby reaction of intermediates ii-e and ii-b at 0-100° C. in propersolvent in the presence of proper base. The reaction time is in therange of 30 minutes to 20 hours, generally being 0.5-10 hours. Theproper solvent mentioned may be selected from benzene, toluene, xylene,chloroform, dichloromethane, acetone, butanone, tetrahydrofuran,acetonitrile, 1,4-dioxane, DMF, N-methyl pyrrolidone or DMSO and so on.Proper base mentioned may be selected from alkali metal hydride such assodium hydride; alkali metal hydroxides such as sodium hydroxide orpotassium hydroxide; alkali carbonate such as sodium carbonate orpotassium carbonate; organic amine such as pyridine or triethylamine.

When L refers to boric acid group. The method to prepare the compoundsrepresented by general formula ii-f refers to the method to prepare thecompounds represented by general formula ii-c with method of cyanoreduction.

The salts represented by general formula ii-g can be prepared bydeprotection reaction of intermediates represented by general formulaii-f and proper acid in proper solvent, and then alkalized to obtainii-1. The preferred temperature is 0-50° C. The reaction time is in therange of 30 minutes to 20 hours, generally being 0.5-10 hours. Theproper solvent mentioned may be selected from ethyl acetate, methylacetate, methyl formate, benzene, toluene, xylene, chloroform,dichloromethane, water, tetrahydrofuran, acetonitrile, 1,4-dioxane, DMF,N-methyl pyrrolidone or DMSO and so on, the proper acid mentioned may beselected from hydrochloric acid, trifluoroacetic acid, sulfuric acid,acetic acid, propionic acid, butyric acid, oxalic acid,

adipic acid, dodecanedioic acid, lauric acid, stearic acid, fumaricacid, maleic acid, benzoic acid or phthalic acid, etc. the proper basementioned may be selected from alkali metal hydride such as sodiumhydride; alkali metal hydroxides such as sodium hydroxide or potassiumhydroxide; alkali carbonate, such as sodium carbonate or potassiumcarbonate; organic amine, such as pyridine or triethylamine. Thedetailed operation refers to the methods described in WO2004093800A andUS20050096485.

Other materials mentioned above, such as the compounds represented bygeneral formula ii-a, ii-b, ii-d and Boc₂O, used to prepare thecompounds represented by general formula ii-1, are commerciallyavailable.

Method 2: when X₁=N, the intermediate ii used to prepare the compoundsrepresented by the general formula III (wherein A=NH) can be preparedaccording to the following two schemes in which B is selected fromdifferent substituent.

(1) When B=—CH₂—, the detailed operation refers to the methods describedin WO9404527, US20110054173 or WO2011025505. The compounds also can beprepared according to the following method.

Wherein, U is a leaving group, selected from halogen or hydroxy, etc.

The intermediates represented by general formula ii-j can be prepared byreaction of intermediates represented by general formula ii-h and ii-iin proper solvent and temperature in the presence of proper base. Thereaction time is in the range of 30 minutes to 20 hours, generally being0.5-10 hours. The intermediates represented by general formula ii-k canbe prepared by reduction reaction of intermediates represented bygeneral formula ii-j and Red-Al, the detailed operation refers to themethods described in EP1840128. The intermediates represented by generalformula ii-L can be prepared by reaction of intermediates represented bygeneral formula ii-k and sulfoxide chloride according to known methods.The intermediates represented by general formula ii-m can be prepared byreaction of intermediates represented by general formula ii-L and sodiumcyanide according to the methods described in WO2007045989 andWO2009115257. According to the methods described in Journal of OrganicChemistry, 71(21), 8023-8027; 2006, Synthesis, (24), 4242-4250, 2010,Heterocycles, 56(1-2), 443-455, 2002 or ARKIVOC (Gainesville, Fla.,United States) [online computer file], (10), 40-51, 2002, Theintermediates represented by general formula ii-n can be prepared viaintermediate ii-m. Finally, the intermediates represented by generalformula ii-2 can be prepared by reaction of intermediates represented bygeneral formula ii-n and ammonia water in the presence of propercatalyst by using hydrogenation reduction. The detailed operation refersto the methods described in J. Am. Chem. Soc, 70, 3788(1948); 82,681(1960); 82, 2386(1960); Can. J. Chem, 49, 2990(1971); J. Org. Chem,37, 335(1972); Organic Syntheses, Coll. Vol. 3, p. 229, p. 720 (1955),Vol. 23, p. 71 (1943) or Vol. 27, p. 18 (1947). The proper catalystsmentioned may be selected from Raney-nickel, palladium carbon orplatinum oxide, etc.

The sources of intermediates are as follows: the intermediaterepresented by general formula ii-h and ii-I are commercially available,or can be prepared according to the conventional method.

The proper base mentioned may be selected from potassium hydroxide,sodium hydroxide, sodium carbonate, potassium carbonate, sodiumbicarbonate, triethylamine, pyridine, sodium methoxide, sodium ethoxide,sodium hydride, potassium tert-butoxide or sodium tert-butoxide and soon.

The reaction was carried out in proper solvent and the proper solventmentioned may be selected from tetrahydrofuran, 1,4-dioxane,acetonitrile, toluene, xylene, benzene, DMF, N-methyl pyrrolidone, DMSO,acetone or butanone and so on.

The proper temperature mentioned is from room temperature to boilingpoint of the solvent, normal temperature is from 20 to 100° C.

The reaction time is in the range of 30 minutes to 20 hours, generallybeing 1-10 hours.

(2) When B=—CH₂CH₂—, the preparation method is as follows:

The compounds represented by general formula ii-o can be prepared byreaction of the compounds represented by general formula ii-n accordingto the methods described in Synthesis, (9), 727-9; 1983 or TetrahedronLetters, 39(51), 9455-9456; 1998; the compounds having general formulaii-3 can be prepared by reaction of the compounds having general formulaii-o according to the methods in which B=—CH₂—.

The second method to prepare the compounds represented by generalformula PY: when A=NR₁₂ (R₁₂≠H), the compounds represented by generalformula PY-2 can be prepared by reaction of the compounds represented bygeneral formula PY-1 with U-R1 according to the conventional method (Udefined as above); or can be prepared according to the methods describedin JP08269021, JP3543411, JP1995-72621, JP1995-96669, JP3511729,JP08291149, EP530149, WO9208704 and WO2004093800A.

The third method to prepare the compounds represented by general formulaPY: when A=O or S, the compounds represented by general formula PY-3,PY-4 can be prepared according to the methods described in WO2012075917and EP534341.

The structural formula of the compounds represented by general formulaPY-2, PY-3 and PY-4 are shown as follows

In general formula PY, the corresponding salts represented by generalformula PY-5A can be prepared by reaction of the compounds representedby general formula PY-5 (when A=NR₁₂) with corresponding organic acidsor inorganic acids, as shown in the following.

In addition, in general formula PY, the salts can also formed based onnitrogen atom of pyrimidine ring, the preparation method refers toDE19647317, JP2001504473, U.S. Pat. No. 5,925,644, WO9822446 andZA9710187, etc.

The reaction forming salts of compounds represented by general formulaPY-5 with organic acids or inorganic acids can be carried out at roomtemperature to boiling point of the solvent, normal temperature is from20 to 100° C. The reaction time is in the range of 30 minutes to 20hours, generally being 1-10 hours. The proper solvent mentioned may beselected from water, methanol, ethanol, isopropanol, benzene, toluene,xylene, acetone, ethyl methyl ketone, methyl isobutyl ketone,chloroform, dichloromethane, methyl acetate, ethyl acetate,tetrahydrofuran, 1,4-dioxane, DMF, N-methyl pyrrolidone or DMSO and soon.

The acids, which can be used to form salts with compounds represented bygeneral formula PY-5, includes carboxylic acid, such as formic acid,acetic acid, propanoic acid, butyric acid, oxalic acid, trifluoroaceticacid, adipic acid, dodecanedioic acid, lauric acid, stearic acid,fumaric acid, maleic acid, sorbic acid, malic acid, citric acid, benzoicacid, p-toluylic acid or phthalic acid, etc. sulfonic acid, such asmethanesulfonic acid, 1, 3-propylene sulfonic acid, p-toluenesulfonicacid or dodecylbenzene sulfonic acid, etc. inorganic acid, such ashydrochloric acid, sulphuric acid, nitric acid, phosphorous acid orcarbonic acid, etc. The further preferred acids are hydrochloric acid,sulphuric acid, nitric acid, phosphorous acid, acetic acid,trifluoroacetic acid, oxalic acid, methanesulfonic acid,p-toluenesulfonic acid or benzoic acid.

Although the compounds represented by general formula PY and somecompounds reported in prior art are both belong to substitutedpyrimidine compounds, there are still some obvious differences instructure between them. It is due to these differences in structure thatlead to compounds of present invention with better fungicidal and/orinsecticidal/acaricidal activities.

The compounds represented by general formula PY show excellent activityagainst both many plant pathogens/diseases in agricultural and otherfields, and insects/mites. Therefore the technical scheme of the presentinvention also includes the uses of the compounds represented by generalformula PY or their salts/complexes to prepare fungicides,insecticides/acaricides in agricultural, forestry or public healthfields. The further preferred technical scheme of the present inventionalso includes the uses of the compounds represented by general formulaI, II or III or their salts/complexes to prepare fungicides,insecticides/acaricides in agricultural, forestry or public healthfields.

The present invention is explained by the following examples of plantdisease and insect pests, but without being restricted thereby.

The compounds represented by general formula PY can be used to controlthese plant diseases: Oomycete diseases, such as downy mildew (cucumberdowny mildew, rape downy mildew, soybean downy mildew, downy mildew ofbeet, downy mildew of sugarcane, tobacco downy mildew, pea downy mildew,vegetable sponge downy mildew, chinese wax gourd downy mildew, muskmelondowny mildew, chinese cabbage downy mildew, spinach downy mildew, radishdowny mildew, grape downy mildew, onion downy mildew), white rust (rapewhite rust, chinese cabbage white rust), damping-off disease (rapedamping-off, tobacco damping-off, tomato damping-off, pepperdamping-off, eggplant damping-off, cucumber damping-off, cottondamping-off), pythium rot (pepper soft stale disease, vegetable spongecottony leak, chinese wax gourd cottony leak), blight (broad beanphytophthora blight, cucumber phytophthora blight, pumpkin phytophthorarot, chinese wax gourd phytophthora blight, watermelon phytophthorablight, muskmelon phytophthora blight, pepper phytophthora blight,chinese chives phytophthora blight, carlic phytophthora blight, cottonphytophthora blight), late blight (potato late blight, tomato lateblight) and so on; diseases caused by Deuteromycotina, such as wiltdisease (sweet potato fusarium wilt, cotton fusarium wilt disease,sesame wilt disease, fusarium wilt disease of costarbean, tomatofusarium wilt, bean fusarium wilt, cucumber fusarium wilt, vegetablesponge fusarium wilt, pumpkin fusarium wilt, chinese wax gourd fusariumwilt, watermelon fusarium wilt, muskmelon fusarium wilt, pepper fusariumwilt, broad bean fusarium wilt, fusarium wilt disease of rape, fusariumwilt disease of soybean), root rot (pepper root rot, eggplant root rot,bean fusarium root-rot, cucumber fusarium root rot, balsam pear fusariumroot rot, cotton black root rot, broad bean thielaviopsis root rot),drooping disease (cotton soreshin, sesame soreshin, pepper rhizoctoniarot, cucumber rhizoctonia rot, chinese cabbage rhizoctonia rot),anthracnose (sorghum anthracnose, cotton anthracnose, kenaf anthracnose,jute anthracnose, flax anthracnose, tobacco anthracnose, mulberryanthracnose, pepper anthracnose, eggplant anthracnose, bean anthracnose,cucumber anthracnose, balsam pear anthracnose, summer squashanthracnose, chinese wax gourd anthracnose, watermelon anthracnose,muskmelon anthracnose, litchi anthracnose), verticillium wilt (cottonverticillium wilt, verticillium wilt of sunflower, tomato verticilliumwilt, pepper verticillium wilt, eggplant verticillium wilt), scab(summer squash scab, chinese wax gourd scab, muskmelon scab), gray mold(cotton boll gray mold, kenaf gray mold, tomato gray mold, pepper graymold, bean gray mold, celery gray mold, spinach gray mold, kiwi fruitgray mold rot), brown spot (cotton brown spot, jute brown spot, beetsercospora leaf spot, peanut brown spot, pepper brown leaf spot, chinesewax gourd corynespora leaf spot, soybean brown spot, sunflower brownspot, pea ascochyta blight, broad bean brown spot), black spot (flaxblack spot, rape alternaria leaf spot, sesame black spot, sunfloweralternaria leaf spot, costarbean alternaria leaf spot, tomato nail headspot, pepper black fruit spot, eggplant black spot, bean leaf spot,cucumber alternaria blight, celery alternaria black leaf spot, carrotalternaria black rot, carrot leaf blight, apple alternaria rot, peanutbrown spot), spot blight (tomato septoria leaf spot, pepper septorialeaf spot, celery late blight), early blight (tomato early blight,pepper early blight, eggplant early blight, potato early blight, celeryearly blight), ring spot (soybean zonate spot, sesame ring spot, beanzonate spot), leaf blight (sesame leaf blight, sunflower leaf blight,watermelon alternaria blight, muskmelon alternaria spot), basal stem rot(tomato basal stem rot, bean rhizoctonia rot), and others (corn northernleaf spot, kenaf damping-off, rice blast, millet black sheath, sugarcaneeye spot, cotton aspergillus boll rot, peanut crown rot, soybean stemblight, soybean black spot, muskmelon alternaria leaf blight, peanut webblotch, tea red leaf spot, pepper phyllosticta blight, chinese wax gourdphyllosticta leaf spot, celery black rot, spinach heart rot, kenaf leafmold, kenaf brown leaf spot, Jute stem blight, soybean cercospora spot,sesame leaf spot, costarbean gray leaf spot, tea brown leaf spot,eggplant cercospora leaf spot, bean cercospora leaf spot, balsam pearcercospora leaf spot, watermelon cercospora leaf spot, jute dry rot,sunflower root and stem rot, bean charcoal rot, soybean target spot,eggplant corynespora leaf spot, cucumber corynespora target leaf spot,tomato leaf mold, eggplant fulvia leaf mold, broad bean chocolate spot)and so on; diseases caused by Basidiomycete, such as rust (wheat striperust, wheat stem rust, wheat leaf rust, peanut rust, sunflower rust,sugarcane rust, chinese chives rust, onion rust, millet rust, soybeanrust), smut (corn head smut, corn smut, sorghum silk smut, sorghum loosekernel smut, sorghum hard smut, sorghum smut, millet kernel smut,sugarcane smut, bean rust), and others (for example, wheat sheath blightand rice sheath blight) and so on; diseases caused by Ascomycete, suchas powdery mildew (wheat powdery mildew, rape powdery mildew, powderymildew of sesame, powdery mildew of sunflower, beet powdery mildew,eggplant powdery mildew, pea powdery mildew, vegetable sponge powderymildew, pumpkin powdery mildew, summer squash powdery mildew, chinesewax gourd, muskmelon powdery mildew, grape powdery mildew, broad beanpowdery mildew), sclerotinia rot (flax sclertiniose, rape sclertiniose,soybean sclertiniose, peanut sclertiniose, tobacco sclerotinia rot,pepper sclerotinia rot, eggplant sclerotinia rot, bean sclerotinia rot,pea sclerotinia rot, cucumber sclerotinia rot, balsam pear sclerotiniarot, chinese wax gourd sclerotinia rot, watermelon sclerotinia disease,celery stem rot), scab (apple scab, pear scab) and so on. Especially,the compounds of the present invention exhibit very good control againstcorn southern rust, rice blast, cucumber gray mold and cucumber downymildew at very low doses.

The compounds represented by general formula PY can be used to controlthese insect pests: Coleoptera, such as Acanthoscelides spp.,Acanthoscelides obtectus, Agrilus planipennis, Agriotes spp.,Anoplophora glabripennis, Anthonomus spp., Anthonomus grandis, Aphidiusspp., Apion spp., Apogonia spp., Atacnius sprctulus, Atomaria linearis,pygmy mangold beetle, Aulacophore spp., Bothynoderes punctiventris,Bruchus spp., Bruchus pisorum, Cacoesia, Cacoesia spp., Callosobruchusmaculatus, Carpophilus hemipteras, Cassida vittata, Cerosterna spp.,Ccrotoma, Ccrotoma spp., Cerotoma trifur cata, Ceutorhynchus spp.,Ceutorhynchus assimilis, cabbage seedpod weevil, Ceutorhynchus napi,cabbage curculio, Chaetocnema spp., Colaspis spp., Conoderus scalaris,Conoderus stigmosus, Conotrachelus nenuphar, Cotinus nitidis, Green Junebeetle, Crioceris asparagi, Cryptolestes ferrugincus, rusty grainbeetle,Cryptolestes pusillus, Cryptolestes turcicus Turkish grain beetle,Ctenicera spp., Curculio spp., Cyclocephala spp., Cylindrocpturusadspersus, sunflower stem weevil, Deporaus marginatus, mangoleaf-cutting weevil, Dermestes lardarius, Dermestes maculates,Diabrotica spp., Epilachna varivcstis, raustinus cubae, Hylobius pales,pales weevil, Hypera spp., Hypera postica, Hyperdoes spp., Hyperodesweevil, Hypothenemus hampei, Ips spp., engravers, Lasioderma serricorne,Leptinotarsa decemlineata, Liogenys fuscus, Liogenys suturalis,Lissorhoptrus oryzophilus, Lyctus spp., powder post beetles, Maecolaspisjoliveti, Megascelis spp., Melanotus communis, Meligethes spp.,Meligethes aeneus, blossom beetle, Melolontha melolontha, Oberea brevis,Oberea linearis, Oryctes rhinoceros, date palm beetle, Oryzaephilusmercator, merchant grain beetle, Oryzaephilus surinamensis, sawtoothedgrain beetle, Otiorhynchus spp., Oulema melanopus, cereal leafbeetle,Oulema oryzae, Pantomorus spp., Phyllophaga spp., Phyllophaga cuyabana,Phyllotreta spp., Phynchites spp., Popillia japonica, Prostephanustruncates, larger grain borer, Rhizopertha dominica, lesser grain borer,Rhizotrogus spp., Eurpoean chafer, Rhynchophorus spp., Scolytus spp.,Shenophorus spp. Sitona lincatus, pca leaf weevil, Sitophilus spp.,Sitophilus granaries, granary weevil, Sitophilus oryzae, rice weevil,Stegobium paniceum, drugstore beetle, Tribolium spp., Triboliumcastaneum, red flour beetle, Tribolium confusum, confused flour beetle,Trogoderma variabile, warehouse beetle and Zabrus tenebioides.

Dermaptera.

Dictyoptera, such as Blattella germanica, German cockroach, Blattaorientalis, Parcoblatta pennylvanica, Periplaneta americana, Americancockroach, Periplaneta australoasiae, Australian cockroach, Periplanctabrunnca, brown cockroach, Periplaneta fuliginosa, smokybrown cockroach,Pyncoselus suninamensis, Surinam cockroach and Supella longipalpa,brownbanded cockroach.

Diptera, such as Aedes spp., Agromyza frontella, alfalfa blotchleafminer, Agromyza spp., Anastrepha spp., Anastrepha suspensa,Caribbean fruit fly, Anopheles spp., Batrocera spp., Bactroceracucurbitae, Bactrocera dorsalis, Ceratitis spp., Ceratitis capitata,Chrysops spp., Cochliomyia spp., Contarinia spp., Culex spp., Dasineuraspp., Dasineura brassicae, Delia spp., Delia platura, seedcom maggot,Drosophila spp., Fannia spp., Fannia canicularis, little house fly,Fannia scalaris, Gasterophilus intestinalis, Gracillia perseae,Haematobia irritans, Hylemyia spp., root maggot, Hypoderma lineatum,common cattle grub, Liriomyza spp., Liriomyza brassica, serpentineleafminer, Melophagus ovinus, Musca spp., muscid fly, Musca autumnalis,face fly, Vusca domestica, house fly, Oestrus ovis, sheep bot fly,Oscinella frit, Pegomyia betae, beet leafminer, Phorbia spp., Psilarosae, carrotrust fly, Rhagoletis cerasi, cherry fruit fly, Rhagoletispomonella, apple maggot, Sitodiplosis mosellana, orange wheat blossommidge, stomoxys calcitruns, stable fly, Tahanus spp. and Tipula spp.

Hemiptera, such as Acrosternum hilare, green stink bug, Blissusleucopterus, chinch bug, Calocoris norvegicus, potato mirid, Cimexhemipterus, tropical bed bug, Cimex lectularius, bed hug, Daghertusfasciatus, Dichelops furcatus, Dysdercus suturellus, cotton stainer,Edessa meditabunda, Eurygaster maura, cereal bug, Euschistus heros,Euschistus servus, brown stink bug, Helopeltis antonii, Helopeltistheivora, tea blight plantbug, Lagynotomus spp., Leptocorisa oratorius,Leptocorisa varicomi, Lygus spp., plant bug, Lygus hesperus, westerntarnished plant bug, Maconellicoccus hirsutus, Neurocolpus longirostris,Nezara viridula, southern green stink bug, PhyLocoris spp., Phytocoriscalifornicus, Phytocoris relativus, Piezodorus guildingi, Poecilocapsuslineatus, fourlined plant bug, Psallus vaccinicola, Pseudacysta perseae,Scaptocoris castanea and Triatoma spp., bloodsuckingconenose bug,kissing bug.

Homoptera, such as Acrythosiphonpisum, pea aphid, Adelges spp.,adelgids, Aleurodes proletella, Aleurodicus disperses, Aleurothrixusflccosus, woolly whitefly, Aluacaspis spp., Amrasca bigutella bigutella,Aphrophora spp., leafhopper, Aonidiella aurantii, California red scale,Aphis spp., Aphis gossypii, cotton aphid, Aphis pomi, apple aphid,Aulacorthitm solan, foxglove aphid, Bemisia spp., Bemisia argentifolii,Bemisia tabaci, sweetpotato whitefly, Brachycolus noxius, Russian aphid,Brachycorynclia asparagi, asparagus aphid, Brevennia rehi, Brevicorynebrassicae, Ceroplastes spp., Ceroplastes rubens, red wax scale,Chionaspis spp., Chrysomphalus spp., Coccus spp., Dysaphis plantaginea,rosy apple aphid, Empoasca spp., Eriosoma lanigerum, woolly apple aphid,Icerya purchasi, cottony cushion scale, Idioscopus nitidulus, mangoleafhopper, Laodelphax striatellus, smaller brown planthopper,Lepidosaphes spp., Macrosiphum spp., Macrosiphum euphorbiae, potatoaphid, Macrosiphum granarium, English grain aphid, Macrosiphum rosae,rose aphid, Macrosteles quadrilineatus, aster leafhopper, Mahanarvafrimbiolata, Metopolophium dirhodum, rose grain aphid, Midislongicornis, Myzus persicae, green peach aphid, Nephotettix spp.,Nephotettix cinctipes, green leafhopper, Nilaparvata lugens, brownplanthopper, Parlatoria pergandii, chaff scale, Parlatoria ziziphi,ebony scale, Peregrinus maidis, corn delphacid, Philaenus spp.,Phylloxera vitifoliae, grape phylloxera, Physokermes piceae, spruce budscale, Planococcus spp., Pseudococcus spp., Pseudococcus brevipes, pineapple mealybug, Quadraspidiotus perniciosus, San Jose scale,Rhapalosiphum spp., Rhapalosiphum maida, corn leaf aphid, Rhapalosiphumpadi, oatbird-cherry aphid, Saissetia spp., Saissetia oleae, Schizaphisgraminum, greenbug, Sitobion avenge, Sogatella furcifera, white-backedplanthopper, Therioaphis spp., Toumeyella spp., Toxoptera spp.,Trialeurodes spp., Trialeurodes vaporariorum, greenhouse whitefly,Trialeurodes abutiloneus, bandedwing whitefly, Unaspis spp., Unaspisyanonensis, arrowhead scale and Zulia entreriana.

Hymenoptera, such as Acromyrrmex spp., Athalia rosae, Atta spp.,leafcutting ants, Camponotus spp., carpenter ant, Diprion spp., sawfly,Formica spp., Iridomyrmex humilis, Argentineant, Monomorium ssp.,Monomorium minumum, little black ant, Monomorium pharaonis, haraoh ant,Neodiprion spp., Pogonomyrmex spp., Polistes spp., paper wasp,Solenopsis spp., Tapoinoma sessile, odorous house ant, Tetranomoriumspp., pavement ant, Vespula spp., yellow jacket and Xylocopa spp.,carpenter bee.

Isoptera, such as Coptotermes spp., Coptotermes curvignathus,Coptotermes frenchii, Coptotermes formosanus, Formosan subterraneantermite, Cornitermes spp., nasute termite, Cryptotermes spp.,Heterotermes spp., desert subterranean termite, Ileterotermes aureus,Kalotermes spp., Incistitermes spp., Macrotermes spp., fungus growingtermite, Marginitermes spp., Microcerotermes spp., harvester termite,Microtermes obesi, Procornitermes spp., Reticulitermes spp.,Reticulitermes banyulensis, Reticulitermes grassei, Reticulitermesflavipes, Reticulitermes hageni, Reticulitermes hesperus, Reticulitermessantonensis, Reticulitermes speratus, Reticulitermes tibialis,Reticulitermes virginicus, Schedorhinotermes spp. and Zootermopsis spp.

Lepidoptera, such as Achoea janata, Adoxophyes spp., Adoxophyes orana,Agrotis spp., Agrotis ipsilon, Alabama argillacea, cotton leafworm,Amorbia cuneana, Amyelosis transitella, navel orangeworm, Anacamptodesdefectaria, Anarsia lineatella, peach twig borer, Anomis sabulijera,jute looper, Anticarsia gemmatalis, velvetbean caterpillar, Archipsargyrospila)(fruit tree leafroller, Archips rosana, rose leaf roller, Argyrotaenia spp., tortricid moths, Argyrotaenia citrana, orange tortrix,Autographa gamma, Bonagota cranaodcs, Borbo cinnara, rice leaf folder,Bucculatrix thurberiella, cotton leafperforator, Caloptilia spp., Capuareticulana, Carposina niponensis, peach fruit moth, Chilo spp.,Chlumetia transversa, mango shoot borer, Choristoneura rosaceana,oblique banded leaf roller, Chrysodeixis spp., Cnaphalocerus medinalis,grass leafroller, Colias spp., Conpomorpha cramerella, Cossus cossus,Crambus spp., Sod webworms, Cydia funebrana, plum fruit moth, Cydiamolesta, oriental fruit moth, Cydia nignicana, pea moth, Cydiapomonella, codling moth, Darna diducta, Diaphania spp., stem borer,Diatr aea spp., stalk bor er, Diatraea saccharalis, sugarcane borer,Diatraea graniosella, southwester corn borer, Earias spp., Eariasinsulata, Egyptian bollworm, Earias vit.ella, rough northern bollworm,Ecdytopopha aurantianum, Elasmopalpus lignosellus, lesser cornstalkborer, Epiphysias postruttana, light brown, apple moth, Ephestia spp.,Ephestia cautella, almond moth, Ephestia elutella, tobbaco moth,Ephestia kuehniella, Mediterranean flour moth, Epimeces spp, Epinotiaaporema, Erionota thrax, banana skipper, Eupoecilia ambiguella, grapeberry moth, Euxoa auxiliaris, army cutworm, Feltia spp., Gortyna spp.,Grapholita molesta, oriental fruit moth, Hedylepta indicata, bean leafwebber, Helicoverpa spp., Helicoverpa armigera, cotton bollworm,Helicoverpa zea, Heliothis spp., Heliothis virescens, tobacco budworm,Hellula undalis, cabbage webworm, Indarbela spp. Keiferialycopersicella, tomato pinworm, Leucinodes orbonalis, eggplant fruitborer, Leucoptera malifoliella, Lithocollectis spp., Lobesia botrana,grape fruit moth, Loxagrotis spp., Loxagrotis albicosta, western beancutworm, Lymantria dispar, gypsy moth, Lyonetiaclerkella, appleleafminer, Mahasena corbetti, oil palm bagworm, Malacosoma spp., tentcaterpillars, Mamestra brassicae, cabbage armyworm, Maruca testulalis,Metisa plana, Mythimna unipuncta, true armyworm, Neoleucinodeselegantalis, small tomato borer, Nymphula depunctalis, rice caseworm,Operophthera brumata, winter moth, Ostrinia nubilalis, European cornborer, Oxydia vesulia, Pandemis cerasana, common currant tortrix,Pandemis heparana, brown apple tortrix, Papilio demodocus, Pectinophoragossypiella, pink bollworm, Peridroma spp., Peridroma saucia, variegatedcutworm, Perileucoptera coffeella, white coffee leafminer, Phthorimaeaoperculella, potato tuber moth, Phyllocnisitis citrella, Phyllonorycterspp., Pieris rapae, imported cabbageworm, Plathypena scabra, Plodiainterpunctella, Indian meal moth, Plutella xylostella, diamondback moth,Polychrosis viteana, grape berry moth, Prays endocarps, Prsys oleae,olive moth, Pseudaletia spp., Pseudaletia unipunctata, Pseudoplusiaincludens, soybean looper, Rachiplusia nu, Scirpophaga incertulas,Sesamia spp., Sesamia inferens, pink rice stemborer, Sesamianonagrioides, Setora nitens, Sitotroga cerealella, Angoumois grain moth,Sparganothis pilleriana, Spodoptera spp., Spodoptera exigua, beetarmyworm, Spodoptera fugiperda, fall armyworm, Spodoptera oridania,southern armyworm, Synanthedon spp., Thecla basilides, Thermisiagemmatalis, Tineola bisselliella, webbing clothes moth, Trichoplusia ni,cabbage looper, Tuts absoluta, Yponomeuta spp., Zeuzeracoffeae, redbranch borer and Zeuzera pyrina, eopard moth.

Mallophaga, chewing lice, such as Bovicola ovis, sheep biting louse,Menacanthus stramineus, chicken body louse and Menopon gallinea, commonhen house,

Orthoptera, such as Anabrus simplex, Mormon cricket, Gryllotalpidae,mole cricket, Locusta migratoria, Melanoplus spp., Microcentrumretinerve, angular winged katydid, Pterophylla spp., histocercagregaria, Scudderia furcata, fork tailed bush katydid and Valanganigricorni, sucking louse, such as Haematopinus spp., Linognathusovillus, sheep louse, Pediculus humanus capitis, Pediculus humanushumanus and Pthirus pubis, crab louse.

Siphonaptera, such as Ctenocephal ides canis, dog flea, Ctenocephalidesfelis, cat flea and Pulex irritanshuman flea.

Thysanoptera, such as Frankliniella fusca, tobacco thrip, Frankliniellaoccidentalis, western flower thrips, Frankliniella shultzei,Frankliniella williamsi, corn thrip, IIeliothrips haemorrhaidalis,greenhouse thrip, Riphiphorothrips cruentatus, Scirtothrips spp,Scirtothrips cirri, citrus thrip, Scirtothrips dorsalis, yellow teathrips, Taeniothrips rhopalantennalis and Thrips spp.

Thysanura, bristletail, such as Lepisma spp, silverfish and Thermobiaspp.

Acarina, mite and tick, such as Acarapsis woodi, tracheal mite ofhoneybee, Acarus spp., Acarus siro, grain mite, Aceria mangiferae, mangobud mite, Aculops spp., Aculops lycopersici, tomato russet mite, Aculopspelekasi, Aculus pelekassi, Aculus schlechtendali, apple rust mite,Amblyomma americanum, lone star tick, Boophilus spp., Brevipalpusobovatus, privet mite, Brevipalpus phoenicis, red and black flat mite,Demodex spp., mange mites, Dermacentor spp., Dermacentor variabilis,american dog tick, Dermatophagoides pteronyssinus, house dust mite,Eotetranycus spp., Eotetranychus carpini, yellow spider mite, Epitimerusspp., Eriophyes spp.,

; odes spp., Metatetranycus spp., Notoedres cati, Oligonychus spp.,Oligonychus coffee, Oligonychus ilicus, southernred mite, anonychusspp., Panonychus cirri, citrus red mite, Panonychus ulmi, European redmite, Phyllocoptruta oleivora, citrus rust mite, Polyphagotarsonemunlatus, broad mite, Rhipicephalus sanguineus, brown dog tick,Rhizoglyphus spp., bulb mite, Sarcoptes scabiei, itch mite, Tegolophusperseaflorae, Tetranychus spp., Tetranychus urticae, twospotted spidermite and Varroa destructor.

Nematoda, such as Aphelenchoides spp., bud and leaf & pine woodnematode, Belonolaimus spp., sting nematodes, Criconemella spp., ringnematodes, Dirofilaria immitis, dog heartworm, Ditylenchus spp.,Heterodera spp., cyst nematode, Heterodera zeae, corn cyst nematode,Hirschmanniella spp., root nematodes, Hoplolaimus spp., lance nematodes,Meloidogyne spp., Meloidogyne incognita, Onchocerca volvulus, hook-tailworm, PraLylenchus spp., lesion nematode, Radopholus spp., burrowingnematode and Rotylenchus reniformis, kidney-shaped nematode.

Symphyla, such as Scutigerella immaculata.

Especially, the compound represented by the present invention providesgreat control effects against peach aphid, diamondback moth, armyworm,and carmine spider mite, and acquires great effects at a minimal dosage.

Due to their positive characteristics, the compounds mentioned above canbe advantageously used in protecting crops of farming and gardening,domestic and breeding animals, as well as environments frequented byhuman beings, from pathogens, insects and pest mites.

In order to obtain desired effect, the dosage of the compound to beapplied can vary with various factors, for example, the used compound,the protected crop, the type of harmful organism, the degree ofinfestation, the climatic conditions, the application method and theadopted formulation.

The dosage of compounds in the range of 10 g to 5 kg per hectare canprovide a sufficient control.

A further object of the present invention also includes fungicidal,insecticidal/acaricidal compositions containing the compounds havinggeneral formula PY as active ingredient, and the weight percentage ofthe active ingredient in the composition is 0.1-99%. The fungicidal,insecticidal/acaricidal compositions also include the carrier beingacceptable in agriculture, forestry, public health.

Especially, a preferred object of the present invention also includesfungicidal, insecticidal/acaricidal compositions containing thecompounds and its salts/complexes having general formula I, II or III asactive ingredient, wherein the weight percentage of the activeingredient in the composition is 0.1-99%.

The compositions of the present invention can be used in the form ofvarious formulations. Usually, the compounds having general formula PYas active ingredient can be dissolved in or dispersed in carriers ormade to a formulation so that they can be easily dispersed as anfungicide or insecticide. For example: these chemical formulations canbe made into wettable powder, oil miscible flowable, aqueous suspension,aqueous emulsion, aqueous solution or emulsifiable concentrates.Therefore, in these compositions, at least a liquid or solid carrier isadded, and usually suitable surfactant(s) can be added when needed.

Still also provided by the present invention are the application methodsfor controlling phytopathogenic fungi, insects, pest mites: which is toapply the compositions of the present invention to the phytopathogenicfungi, insects, pest mites as mentioned above or their growing loci. Thesuitable effective dosage of the compounds of the present invention isusually within a range of 10 g/ha to 1000 g/ha, preferably from 20 g/hato 500 g/ha. For some applications, one or more other fungicides,insecticides/acaricides, herbicides, plant growth regulators orfertilizer can be added into the fungicidal, insecticidal/acaricidalcompositions of the present invention to make additional merits andeffects.

It should be noted that variations and changes are permitted within theclaimed scopes in the present invention.

DETAILED DESCRIPTION OF THE INVENTION

The present invention is illustrated by the following examples, butwithout being restricted thereby. (All raw materials are commerciallyavailable unless otherwise specified.)

PREPARATION EXAMPLES Example 1: The Preparation of Intermediate4,5-dichloro-6-methylpyrimidine 1) The Preparation of4-hydroxyl-5-chloro-6-methylpyrimidine

8.80 g (0.16 mol) of CH₃ONa in methanol was added slowly to a solutionof 11.30 g (0.11 mol) of formimidamide in 50 mL of methanol at roomtemperature under stirring, the mixture was stirred for another 2 hrsafter addition at room temperature. Followed by addition of 11.17 g(0.068 mol) of ethyl 2-chloro-3-oxobutanoate, the mixture was continuedstirring for another 5-7 hrs at room temperature. After the reaction wasover by Thin-Layer Chromatography monitoring, the reaction mixture wasconcentrated under reduced pressure and pH was adjusted to 5-6 with HCl,and then filtered to afford orange-yellow solid, the water phase wasextracted with ethyl acetate (3×50 mL), dried over anhydrous magnesiumsulfate, filtered and then concentrated under reduced pressure. Theresidue was dissolved to 50 ml of ethyl acetate, stand overnight toobtain 6.48 g as orange-yellow solid with yield of 66%. m.p. 181-184° C.

2) The Preparation of Intermediate 4,5-dichloro-6-methylpyrimidine

50 ml of POCl₃ was added dropwise to a solution of 14.5 g (0.1 mol) of4-hydroxyl-5-chloro-6-methylpyrimidine in 50 mL of toluene, the mixturewas refluxed for 5-7 hrs after addition. After the reaction was over byThin-Layer Chromatography monitoring, the reaction mixture wasconcentrated under reduced pressure to remove toluene and extra POCl₃,and then poured into ice water. The water phase was extracted with ethylacetate (3×50 mL), the organic phases were emerged, dried over anhydrousmagnesium sulfate, filtered and then concentrated under reducedpressure. The residue was purified through silica column to give 14.43 gas yellow liquid with yield of 88.5%.

Example 2: The Preparation of Intermediate4,5-dichloro-6-(difluoromethyl)pyrimidine 1) The Preparation of2-dichloro-4,4-difluoro-3-oxobutanoate

177.46 g (1.33 mol) of sulfonyl chloride in 200 mL dichloromethane wasadded slowly to a solution of 200.00 g (1.20 mol) of ethyl4,4-difluoro-3-oxobutanoate in 300 mL of dichloromethane at roomtemperature under stirring for 3 hrs, then a lot of gas released outafter addition, the mixture was continued stirring for another 5-7 hrsat room temperature. After the reaction was over by Thin-LayerChromatography monitoring, the excess solvent and sulfonyl chloride wereconcentrated under reduced pressure to obtain 240 g as faint yellowliquid.

2) The Preparation of 4-hydroxyl-5-chloro-6-(difluoromethyl)pyrimidine

A solution of 71.9 g (0.70 mol) of formimidamide in 150 mL of methanolwas stirred at 5-10° C., 64.6 g (1.20 mol) of CH₃ONa in methanolprepared and cooled to room temperature ahead of time was added slowlyto the above solution under stirring, followed by addition of 100 g(0.50 mol) of ethyl 2-chloro-4,4-difluoro-3-oxobutanoate in 100 ml ofmethanol, the mixture was continued stirring for another 3-4 hrs at roomtemperature. After the reaction was over by Thin-Layer Chromatographymonitoring, the reaction mixture was concentrated under reduced pressureand pH was adjusted to 5-6 with HCl, and then filtered to afford 65 g aswhite solid with yield of 73%. m.p. 204-206° C.

3) The Preparation of 4,5-dichloro-6-(difluoromethyl)pyrimidine

100 ml of POCl₃ was added dropwise to a solution of 65.0 g (0.36 mol) of4-hydr oxyl-5-chloro-6-(difluoromethyl)pyrimidin in 150 mL of toluene,the mixture was refluxed for 3-5 hrs after addition. After the reactionwas over by Thin-Layer Chromatography monitoring, the reaction mixturewas concentrated under reduced pressure to remove toluene and extraPOCl₃, and then poured into ice water. The water phase was extractedwith ethyl acetate (3×50 mL), the organic phases were emerged, washedwith saturated sodium bicarbonate, dried over anhydrous magnesiumsulfate, filtered and then concentrated under reduced pressure. Theresidue was purified through silica column to give 64.5 g as yellowliquid, cooled to be solid in refrigerator with yield of 9 0%.

Example 3: The Preparation of2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine 1) ThePreparation of2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)acetonitrile

To a solution of 2-chloro-5-(trifluoromethyl)pyridine 18.15 g (0.1 mol)and 2-(4-hydroxyphenyl)acetonitrile 15.96 g (0.12 mol) in 200 mLbutanone was added potassium carbonate 27.60 g (0.2 mol). The reactionmixture was continued stirring and heating to reflux for 4-10 hrs, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure. Thenthe mixture was poured into 200 mL of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of 5% aqueoussolution of NaOH, and 50 mL of brine successively, dried and evaporatedunder reduced pressure, the residual was purified via silica column(ethyl acetate/petroleum ether (boiling point range 60-90° C.)=1:5, asan eluent) to obtain 22.50 g target intermediate as white solid withyield of 81.5%, m.p. 48-49 □.

2) The Preparation of2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine

To a solution of2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)acetonitrile 2.78 g(0.01 mol), Raney nickel (1.0 g) and 10 mL of 25% aqueous ammonia in 50mL ethanol was filled with hydrogen, then the reaction mixture wascontinued stirring at room temperature for 3-15 hrs and monitored by TLCuntil the reaction was over, Raney nickel was filtered, the solution wasconcentrated under reduced pressure to give sticky oil cooled to obtain2.20 g target intermediate as white solid with yield of 78%, m.p. 82-83°C.

Example 4: The Preparation of4-(2-(5-chloro-6-methylpyrimidin-4-ylamino)ethyl)phenol

To a solution of 4-(2-aminoethyl)phenol 1.13 g (0.01 mol) andtriethylamine 2.02 g (0.02 mol) in 50 mL toluene was dropwise added4,5-dichloro-6-methylpyrimidine 1.63 g (0.01 mol). The reaction mixturewas continued stirring for 4-10 hrs, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the excessive solvent wasevaporated under reduced pressure, then the mixture was poured into(3×50 mL) of ethyl acetate to separate the organic layer, the organicphase was washed with 50 mL of brine, dried and evaporated under reducedpressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:3, as aneluent) to obtain 2.10 g target intermediate as white solid with yieldof 88%, m.p. 177-179° C.

Example 5: The Preparation of Intermediate2-(4-(3,5,6-trichloropyridin-2-yloxy)phenyl)ethanamine 1) tert-butyl4-hydroxyphenethylcarbamate

To a solution of 4-(2-aminoethyl)phenol 11.3 g (0.1 mol) and sodiumbicarbonate 10.08 g (0.12 mol) in 80 mL tetrahydrofuran was dropwiseadded di-tert-butyl dicarbonate 21.80 g (0.1 mol) at room temperature,then the reaction mixture was continued stirring for 4-10 hrs, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure. Thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 17.15 g target intermediate as whitesolid with yield of 81%, m.p. 48-49° C.

-   -   2) The Preparation of tert-butyl        4-(3,5,6-trichloropyridin-2-yloxy)phenethylcarbamate

To a solution of tert-butyl 4-hydroxyphenethylcarbamate 2.37 g (0.01mol) and 2,3,5,6-tetrachloropyridine 2.17 g (0.01 mol) in 50 mL butanonewas added potassium carbonate 2.76 g (0.02 mol). The reaction mixturewas continued stirring and heating to reflux for 4-10 hrs, and monitoredby TLC (Thin-Layer Chromatography) until the reaction was over, theexcessive solvent was evaporated under reduced pressure, then themixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:5, as an eluent) to obtain 3.55 g target intermediate as whitesolid with yield of 82%, m.p. 48-49° C.

3) The Preparation of2-(4-(3,5,6-trichloropyridin-2-yloxy)phenyl)ethanamine hydrochloride

To a solution of tert-butyl4-(3,5,6-trichloropyridin-2-yloxy)phenethylcarbamate 4.17 g (0.01 mol)in 50 mL ethyl acetate was dropwise added 15 mL concentratedhydrochloric acid. The reaction mixture was Gradually dissolved andcontinued stirring for 4-5 hrs, then a large amount of solid wasprecipitated and filtered, the filter cake was washed with 50 mL ethylacetate to obtain 3.0 g target intermediate as white solid with yield of88%, m.p. 48-49° C.

Example 6: The Preparation of Compound I-22

To a solution of 4,5-dichloro-6-methylpyrimidine 1.63 g (0.01 mol) and2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine 2.82 g (0.01mol) in 50 mL toluene was added triethylamine 2.02 g (0.02 mol) afterthe reaction mixture was dissolved. The reaction mixture was continuedstirring and heating to reflux for 4-10 hours, and monitored by TLC(Thin-Layer Chromatography) until the reaction was over, the excessivesolvent was evaporated under reduced pressure, then the mixture waspoured into (3×50 mL) of ethyl acetate to separate the organic layer,the organic phase was washed with 50 mL of brine, dried and evaporatedunder reduced pressure, the residual was purified via silica column(ethyl acetate/petroleum ether (boiling point range 60-90° C.)=1:3, asan eluent) to obtain 3.25 g compound I-22 as white solid with yield of80%, m.p. 98-99° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ(ppm): 2.46 (3H,s), 2.97 (2H, t), 3.79 (2H, q), 5.47 (1H, t), 7.01 (1H, d), 7.12 (2H,d), 7.29 (2H, d), 7.90 (1H, d), 8.40 (1H, d), 8.44 (1H, s).

Example 7: The Preparation of Compound I-254

To a solution of 1.77 g (0.01 mol) 4,5-dichloro-6-ethylpyrimidine (thepreparation refers to Example 1, the difference is replacing ethyl2-chloro-3-oxobutanoate to ethyl 2-chloro-3-oxopentanoate) and2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine 2.82 g (0.01mol) in 50 mL toluene was added triethylamine 2.02 g (0.02 mol). Thereaction mixture was heated to reflux for 4-10 hours, and monitored byTLC (Thin-Layer Chromatography) until the reaction was over, theexcessive solvent was evaporated under reduced pressure, then themixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:3, as an eluent) to obtain 3.56 g compound I-254 as white solidwith yield of 83%, m.p. 76˜78° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ(ppm): 1.26 (3H,t), 2.79 (2H, q), 2.77 (4H, m), 2.97 (2H, t), 3.79 (2H, q), 5.51 (1H,t), 7.00 (1H, d), 7.11 (2H, d), 7.29 (2H, d), 7.89 (1H, d), 8.44 (2H,m).

Example 8: The Preparation of Compound I-483

To a solution of 4-(2-(5-chloro-6-methylpyrimidin-4-ylamino)ethyl)phenol2.64 g (0.01 mol) and2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine 2.33 g (0.01mol) in 30 mL N,N-dimethyl formamide was added potassium carbonate 2.76g (0.02 mol). The reaction mixture was heated to reflux for 4-10 hours,and monitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 3.77 g compound I-483 as colorless oilwith yield of 82%.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.45(3H, s), 2.96 (2H, t), 3.72-3.84 (2H, q), 5.45 (1H, t), 7.13 (2H, d),7.29 (2H, d), 7.99 (1H, d), 8.27 (1H, s), 8.40 (1H, s).

Example 9: The Preparation of Compound I-583

To a solution of 2.78 g (0.01 mol)4-(2-(5-chloro-6-ethylpyrimidin-4-ylamino)ethyl)phenol (the preparationrefers to Example 3, the difference is replacing4,5-dichloro-6-methylpyrimidine to 4,5-dichloro-6-ethylpyrimidine) and2,3,5-trichloropyridine 1.83 g (0.01 mol) in 30 mL N,N-dimethylformamide was added potassium carbonate 2.76 g (0.02 mol). The reactionmixture was heated to reflux for 4-10 hours, and monitored by TLC(Thin-Layer Chromatography) until the reaction was over, the excessivesolvent was evaporated under reduced pressure, then the mixture waspoured into (3×50 mL) of ethyl acetate to separate the organic layer,the organic phase was washed with 50 mL of brine, dried and evaporatedunder reduced pressure, the residual was purified via silica column(ethyl acetate/petroleum ether (boiling point range 60-90° C.)=1:3, asan eluent) to obtain 3.50 g compound I-583 as colorless oil with yieldof 83%, m.p. 53-54° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.26(3H, t), 2.79 (2H, q), 2.96 (2H, q), 3.77 (2H, q), 5.47 (1H, t), 7.11(2H, d), 7.28 (2H, d), 7.77 (1H, s), 8.45 (1H, s).

Example 10: The Preparation of Compound I-2342

To a solution of 4,5-dichloro-6-(difluoromethyl)pyrimidine 1.99 g (0.01mol) and 2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine 2.82g (0.01 mol) in 50 mL toluene was added triethylamine 2.02 g (0.02 mol)after the reaction mixture was dissolved. The reaction mixture wascontinued stirring and heating to reflux for 4-10 hours, and monitoredby TLC (Thin-Layer Chromatography) until the reaction was over, theexcessive solvent was evaporated under reduced pressure, then themixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 3.82 g compound I-2342 as white solidwith yield of 86%, m.p. 102-103° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 8.581(s, 1H, pyrimidine-H), 8.439 (s, 1H, pyridine-6-H), 7.891-7.927 (d, 1H,pyridine-4-H), 7.008-7.037 (d, 1H, pyridine-3-H), 7.111-7.310 (dd, 4H,Ar—H), 6.547-6.904 (t, 1H, F₂C—H, 5.747 (s, 1H, NH), 3.815-3.882 (q, 2H,N—CH₂—C), 2.964-3.010 (t, 2H, C—CH₂—Ar).

Example 11: The Preparation of Compound I-2574

To a solution of 1.99 g (0.01 mol)4,5-dichloro-6-(difluoromethyl)pyrimidine and 2.82 g (0.01 mol)2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine (thepreparation refers to Example 3) in 50 mL toluene was addedtriethylamine 2.02 g (0.02 mol) after the reaction mixture wasdissolved. The reaction mixture was heated to reflux for 4-10 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 4.16 g compound I-2574 as white solidwith yield of 84%.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): δ 8.577(s, 1H, pyrimidine-H), 8.270 (s, 1H, pyridine-6-H), 7.981-7.987 (d, 1H,pyridine-4-H), 7.128-7.319 (dd, 4H, Ar—H), 6.716 (t, 1H, F₂C—H),3.843-3.864 (q, 2H, N—CH₂—C), 2.970-3.016 (t, 2H, C—CH₂—Ar).

Example 12: The Preparation of Compound I-2748

To a solution of 2.17 g (0.01 mol)4,5-dichloro-6-(trifluoromethyl)pyrimidine (the preparation refers toExample 1) and 3.19 g (0.01 mol)2-(4-(5-(trifluoromethyl)pyridin-2-yloxy)phenyl)ethanamine in 50 mLtoluene was added triethylamine 2.02 g (0.02 mol). The reaction mixturewas heated to reflux for 4-10 hours, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the excessive solvent wasevaporated under reduced pressure, then the mixture was poured into(3×50 mL) of ethyl acetate to separate the organic layer, the organicphase was washed with 50 mL of brine, dried and evaporated under reducedpressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:4, as aneluent) to obtain 4.07 g compound I-2748 as white solid with yield of88%, m.p. 96-97° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 8.577(s, 1H, pyrimidine-H), 8.436 (s, 1H, pyridine-6-H), 7.892-7.920 (d, 1H,pyridine-4-H), 7.010-7.039 (d, 1H, pyridine-3-H), 7.115-7.313 (dd, 4H,Ar—H), 5.898 (s, 1H, NH), 3.825-3.890 (q, 2H, N—CH₂—C), 2.966-3.014 (t,2H, C—CH₂—Ar).

Example 13: The Preparation of Compound I-3309

To a solution of 1.77 g (0.01 mol) 4,5-dichloro-6-ethylpyrimidine and2.50 g (0.01 mol) 2-(4-(6-chloropyridazin-3-yloxy)phenyl)ethanamine (thepreparation refers to Example 3, the difference is replacing2-chloro-5-(trifluoromethyl)pyridine to 3,6-dichloropyridazine) in 50 mLtoluene was added 2.02 g (0.02 mol)triethylamine after the reactionmixture was dissolved. The reaction mixture was heated to reflux for4-10 hours, and monitored by TLC (Thin-Layer Chromatography) until thereaction was over, the excessive solvent was evaporated under reducedpressure, then the mixture was poured into (3×50 mL) of ethyl acetate toseparate the organic layer, the organic phase was washed with 50 mL ofbrine, dried and evaporated under reduced pressure, the residual waspurified via silica column (ethyl acetate/petroleum ether (boiling pointrange 60-90° C.)=1:3, as an eluent) to obtain 3.40 g compound I-3309 aswhite solid with yield of 87%, m.p. 138-140° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.25(3H, t), 2.79 (2H, q), 2.96 (2H, t), 3.78 (2H, q), 5.50 (1H, s), 7.16(3H, m), 7.26 (2H, m), 7.50 (1H, d), 8.45 (1H, s).

Example 14: The Preparation of Compound I-4757

To a solution of 1.63 g (0.01 mol) 4,5-dichloro-6-methylpyrimidine and2.75 g (0.01 mol) 2-(4-(4,6-dimethoxypyrimidin-2-yloxy)phenyl)ethanamine(the preparation refers to Example 3, the difference is replacing2-chloro-5-(trifluoromethyl)pyridine to4,6-dimethoxy-2-(methylsulfonyl)pyrimidine) in 50 mL toluene was added2.02 g (0.02 mol)triethylamine after the reaction mixture was dissolved.The reaction mixture was heated to reflux for 4-10 hours, and monitoredby TLC (Thin-Layer Chromatography) until the reaction was over, theexcessive solvent was evaporated under reduced pressure, then themixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 3.24 g compound I-4757 as white solidwith yield of 81%, m.p. 119-120° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.46(3H, s), 2.95 (2H, t), 3.82 (2H, m), 3.84 (6H, s), 5.43 (1H, s), 5.78(1H, s), 7.26 (4H, m), 8.40 (1H, s).

Example 15: The Preparation of Compound I-6730

To a solution of compound I-22 0.41 g (0.01 mol) in 20 mL ethanol wasdropwise added 10 mL of concentrated hydrochloric acid at roomtemperature, The reaction mixture was heated to reflux for 4-10 hours,and monitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thebrown residue was washed with (3×50 mL) of acetone to obtain 0.33 gcompound I-6730 as white solid with yield of 75%, m.p. 108-110° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ(ppm): 2.49 (3H,s), 2.88 (2H, t), 3.64 (2H, m), 7.08 (2H, d), 7.17 (1H, d), 7.35 (2H,d), 7.37 (1H, m), 8.16 (1H, d), 8.25 (1H, s), 8.50 (1H, s).

Example 16: The Preparation of2-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)ethanamine 1) ThePreparation of2-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)acetonitrile

To a solution of 150 mL N,N-dimethyl formamide was added1,2-dichloro-4-(trifluoromethyl)benzene 25.8 g (0.12 mol),2-(4-hydroxyphenyl)acetonitrile 13.3 g (0.1 mol) and potassium carbonate27.60 g (0.2 mol). The reaction mixture was continued stirring andheating to reflux overnight, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the excessive solvent wasevaporated under reduced pressure. Then the mixture was poured into 300mL of ethyl acetate to separate the organic layer, the organic phase waswashed with 50 mL of 5% aqueous solution of NaOH, and 50 mL of brinesuccessively, dried and evaporated under reduced pressure, the residualwas purified via silica column (ethyl acetate/petroleum ether (boilingpoint range 60-90° C.)=1:4, as an eluent) to obtain 14.55 g targetintermediate as white solid with yield of 46.2%, m.p. 66.2° C.

2) The Preparation of2-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)ethanaminehydrochloride

To a solution of2-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)acetonitrile 3.12 g(0.01 mol), Raney nickel (1.0 g) and 10 mL of 25% aqueous ammonia in 50mL ethanol was filled with hydrogen at high pressure, then the reactionmixture was continued stirring at room temperature for 3 hours andmonitored by TLC until the reaction was over, Raney nickel was filtered,the solution was concentrated under reduced pressure to give stickyliquid. To a solution of the residue was dropwise added 5 mL ofconcentrated hydrochloric acid and stirred for half an hour at roomtemperature until target intermediate precipitated, filtered to obtain3.45 g white solid with yield of 97.9%, m.p. 155.7° C.

Example 17: The Preparation of2-(4-(2,6-dichloro-4-nitrophenoxy)phenyl)ethanamine hydrochloride 1) ThePreparation of tert-butyl4-(2,6-dichloro-4-nitrophenoxy)phenethylcarbamate

To a solution of tert-butyl 4-hydroxyphenethylcarbamate 2.10 g (0.01mol) and 1,3-dichloro-2-fluoro-5-nitrobenzene 2.33 g (0.01 mol) in 50 mLbutanone was added potassium carbonate 2.76 g (0.02 mol). The reactionmixture was continued stirring and heating to reflux for 4-10 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 3.73 g target intermediate as whitesolid with yield of 87.3%, m.p. 149-151° C.

2) The Preparation of2-(4-(2,6-dichloro-4-nitrophenoxy)phenyl)ethanamine

To a solution of tert-butyl4-(2,6-dichloro-4-nitrophenoxy)phenethylcarbamate 4.27 g (0.01 mol) in50 mL ethyl acetate was dropwise added 6 mL trifluoroacetic acid untilthe solid was dissolved at room temperature for 4-5 hours, and monitoredby TLC (Thin-Layer Chromatography) until the reaction was over, theexcessive solvent was evaporated under reduced pressure, then themixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure to give 3.03 g target intermediateas white solid with yield of 92.8%, m.p. 107-109° C.

Example 18: The Preparation of2-(4-(4-(trifluoromethyl)phenoxy)phenyl)ethanamine 1) The Preparation oftert-butyl 4-(4-(trifluoromethyl)phenoxy)phenethylcarbamate

To a solution of 4-(trifluoromethyl)phenylboronic acid 4.56 g (0.024mol) in 50 mL dichloromethane was added 4A molecular sieve powder,Cupric Acetate Anhydrous 3.82 g (0.021 mol), triethylamine 10.1 g (0.1mol), and pyridine 7.9 g (0.1 mol) successively; The reaction mixturewas continued to react overnight, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, filtered and the excessivesolvent was evaporated under reduced pressure, then the mixture waspoured into (3×50 mL) of ethyl acetate to separate the organic layer,the organic phase was washed with 50 mL of brine, dried and evaporatedunder reduced pressure, the residual was purified via silica column(ethyl acetate/petroleum ether (boiling point range 60-90° C.)=1:4, asan eluent) to obtain 5.95 g target intermediate as white solid withyield of 65.1%.

2) The Preparation of 2-(4-(4-(trifluoromethyl)phenoxy)phenyl)ethanaminehydrochloride

To a solution of tert-butyl4-(4-(trifluoromethyl)phenoxy)phenethylcarbamate 3.81 g (0.01 mol) in 50mL ethyl acetate was dropwise added 12 mL concentrated hydrochloricacid. The reaction mixture was continued to stir for 4-5 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thenthe mixture was poured into (3×50 mL) of ethyl acetate to react for halfan hour and filtered to give 2.92 g target intermediate as white solidwith yield of 91.9%.

Example 19: The Preparation of Compound II-69

To a solution of 1.63 g (0.01 mol) 4,5-dichloro-6-methylpyrimidine and3.18 g (0.01 mol) 2-(4-(4-(trifluoromethyl)phenoxy)phenyl)ethanaminehydrochloride in 50 mL toluene was added 4.45 g (0.022mol)triethylamine. The reaction mixture was continued stirring andheating to reflux for 4-10 hours, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the excessive solvent wasevaporated under reduced pressure, then the mixture was poured into(3×50 mL) of ethyl acetate to separate the organic layer, the organicphase was washed with 50 mL of brine, dried and evaporated under reducedpressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:2, as aneluent) to obtain 2.76 g compound II-69 as colourless oil with yield of72.6%.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.46(3H, s), 2.94 (2H, t), 3.77 (2H, q), 5.42 (1H, s), 702 (4H, m), 7.25(2H, m), 7.56 (2H, d), 8.39 (1H, s).

Example 20: The Preparation of Compound II-165

To a solution of 1.63 g (0.01 mol) 4,5-dichloro-6-methylpyrimidine and3.26 g (0.01 mol) 2-(4-(2,6-dichloro-4-nitrophenoxy)phenyl)ethanamine in50 mL toluene was added 4.45 g (0.022 mol)triethylamine. The reactionmixture was continued stirring and heating to reflux for 4-10 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure. Thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:2, as an eluent) to obtain 3.23 g compound II-165 as rufous solidwith yield of 71.2%, m.p. 118-120° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.45(3H, s), 2.91 (2H, t), 3.70-3.85 (2H, q), 5.42 (1H, t), 6.80 (2H, d),7.18 (2H, d), 8.31 (2H, s), 8.38 (1H, s).

Example 21: The Preparation of Compound II-297

To a solution of 1.77 g (0.01 mol) 4,5-dichloro-6-ethylpyrimidine (thepreparation refers to Example 1, the difference is replacing ethyl2-chloro-3-oxobutanoate to ethyl 2-chloro-3-oxopentanoate) and 2.84 g(0.01 mol) 2-(4-(4-chlorophenoxy)phenyl)ethanamine hydrochloride (thepreparation refers to Example 18, the difference is replacing4-(trifluoromethyl)phenylboronic acid to 4-chlorophenylboronic acid) in50 mL toluene was added 4.45 g (0.022 mol)triethylamine. The reactionmixture was continued stirring and heating to reflux for 4-10 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:2, as an eluent) to obtain 3.16 g compound II-297 as rufous solidwith yield of 81.6%, m.p. 84.7° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.26(3H, t), 2.78 (2H, dd), 2.92 (2H, t), 3.75 (2H, dd), 5.45 (1H, t),6.84-7.00 (4H, m), 7.20 (2H, d), 7.29 (2H, d), 8.44 (1H, s).

Example 22: The Preparation of Compound II-303

To a solution of 1.77 g (0.01 mol) 4,5-dichloro-6-ethylpyrimidine and3.19 g (0.01 mol) 2-(4-(3,5-dichlorophenoxy)phenyl)ethanaminehydrochloride (the preparation refers to Example 18, the difference isreplacing 4-(trifluoromethyl)phenylboronic acid to3,5-dichlorophenylboronic acid) in 50 mL toluene was added 4.45 g (0.022mol)triethylamine. The reaction mixture was continued stirring andheating to reflux for 4-10 hours, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the excessive solvent wasevaporated under reduced pressure, then the mixture was poured into(3×50 mL) of ethyl acetate to separate the organic layer, the organicphase was washed with 50 mL of brine, dried and evaporated under reducedpressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:2, as aneluent) to obtain 3.17 g compound II-303 as pale rufous oil with yieldof 75.1%.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.26(3H, t), 2.78 (2H, dd), 2.95 (2H, t), 3.72-3.84 (2H, q), 5.45 (1H, t),6.85 (2H, d), 7.00 (2H, d), 7.25 (2H, d), 8.45 (1H, s).

Example 23: The Preparation of Compound II-347

To a solution of 1.77 g (0.01 mol) 4,5-dichloro-6-ethylpyrimidine and3.18 g (0.01 mol) 2-(4-(4-(trifluoromethyl)phenoxy)phenyl)ethanaminehydrochloride in 50 mL toluene was added 4.45 g (0.022mol)triethylamine. The reaction mixture was continued stirring andheating to reflux for 4-10 hours, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the excessive solvent wasevaporated under reduced pressure, then the mixture was poured into(3×50 mL) of ethyl acetate to separate the organic layer, the organicphase was washed with 50 mL of brine, dried and evaporated under reducedpressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:2, as aneluent) to obtain 3.15 g compound II-347 as white solid with yield of74.8%, m.p. 52.6° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.27(3H, t), 2.78 (2H, q), 2.95 (2H, t), 3.78 (2H, q), 5.42 (1H, s), 7.01(4H, m), 7.24 (2H, m), 7.58 (2H, d), 8.45 (1H, s).

Example 24: The Preparation of Compound II-8915

To a solution of 1.98 g (0.01 mol)4,5-dichloro-6-(difluoromethyl)pyrimidine (the preparation refers toExample 1, the difference is replacing ethyl 2-chloro-3-oxobutanoate toethyl 2-chloro-4,4-difluoro-3-oxobutanoate) and 2.84 g (0.01 mol)2-(4-(4-chlorophenoxy)phenyl)ethanamine hydrochloride in 50 mL toluenewas added 4.45 g (0.022 mol)triethylamine. The reaction mixture wascontinued stirring and heating to reflux for 4-10 hours, and monitoredby TLC (Thin-Layer Chromatography) until the reaction was over, theexcessive solvent was evaporated under reduced pressure, then themixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:2, as an eluent) to obtain 2.89 g compound II-8915 as white solidwith yield of 70.5%, m.p. 98.5° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.94(2H, t), 3.76-3.86 (2H, q), 5.71 (1H, s), 6.72 (1H, t), 6.90-7.05 (4H,m), 7.17-7.32 (4H, m), 8.57 (1H, s).

Example 25: The Preparation of Compound II-10583

To a solution of 1.98 g (0.01 mol)4,5-dichloro-6-(difluoromethyl)pyrimidine (the preparation refers toExample 1, the difference is replacing ethyl 2-chloro-3-oxobutanoate toethyl 2-chloro-4,4-difluoro-3-oxobutanoate) and 3.14 g (0.01 mol)2-(4-(4-chlorophenoxy)-3-methoxyphenyl)ethanamine hydrochloride in 50 mLtoluene was added 4.45 g (0.022 mol)triethylamine. The reaction mixturewas continued stirring and heating to reflux for 4-10 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thenthe mixture was poured into (3×50 mL) of ethyl acetate to separate theorganic layer, the organic phase was washed with 50 mL of brine, driedand evaporated under reduced pressure, the residual was purified viasilica column (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:2, as an eluent) to obtain 2.89 g compound II-10583 as rufous oilwith yield of 76.8%.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.95(2H, t), 3.80-3.92 (5H, m), 5.72 (1H, s), 6.72 (1H, t), 6.75-6.97 (5H,m), 7.20-7.26 (2H, m), 8.58 (1H, s).

Example 26: The Preparation of Compound II-19334

To a solution of compound II-347 0.42 g (0.01 mol) in 20 mL ethanol wasdropwise added 10 mL of concentrated hydrochloric acid at roomtemperature. The reaction mixture was heated to reflux for 4-10 hours,and monitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive solvent was evaporated under reduced pressure, thebrown residue was washed with (3×10 mL) of ethyl acetate to obtain 0.36g compound II-19334 as white solid with yield of 78.1%, m.p. 120.5° C.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.27(3H, t), 2.80-3.09 (4H, m), 3.80 (2H, d), 6.92-7.18 (4H, d), 7.31 (2H,d), 7.67 (2H, d), 8.71 (1H, d), 9.28 (1H, s).

Example 27: The Preparation of2-(6-(4-chlorophenoxy)pyridin-3-yl)ethanamine 1) The Preparation ofmethyl 6-(4-chlorophenoxy)nicotinate

To a solution of 25.6 g (0.2 mol) 4-chlorophenol in 350 mLN,N-dimethylformamide was added 70% sodium hydride 103 g (3.0 mol) inbatches. The reaction mixture was stirred for 4 hours at roomtemperature, then 34.2 g (0.2 mol) methyl 6-chloronicotinate was addedin batches, then the reaction temperature was raised to 100° C. to reactfor 10 hours, and monitored by TLC (Thin-Layer Chromatography) until thereaction was over, the solution was poured into water, extracted withethyl acetate, the organic phase was washed with water, saturated brinesuccessively, dried, filtered and evaporated under reduced pressure, thecooled residual was filtered and washed with petroleum ether, to obtain42.0 g air dried target intermediate as brown solid, m.p. 64-66° C.¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ(ppm): 3.92 (3H,s), 6.75 (1H, d), 6.96 (1H, d), 7.11 (2H, d), 7.37 (2H, d), 8.30 (1H,d), 8.81 (1H, s).

2) The Preparation of (6-(4-chlorophenoxy)pyridin-3-yl)methanol

To a solution of 52.6 g (0.2 mol) methyl 6-(4-chlorophenoxy)nicotinatein 500 mL anhydrous ether was dropwise added 65% Red-Al 74.5 g (0.24mol) in toluene at 0□. then the reaction mixture was stirred for 4 hoursat room temperature, then at 0□, 10% sodium hydroxide solution preparedbeforehand was dropwise added until the reaction solution was clarified,then the reaction temperature was raised to 35 □ to react for 2 hours,and monitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the solution was poured into water, extracted with ethyl acetate,the organic phase was washed with water, saturated brine successively,dried, filtered and evaporated under reduced pressure, the residual waspurified via silica column (ethyl acetate/petroleum ether (boiling pointrange 60-90° C.)=1:3, as an eluent) to obtain 42.2 g target intermediateas white solid, m.p. 100-102° C. ¹H-NMR (300 MHz, internal standard TMS,solvent CDCl₃) δ (ppm): 3.20 (1H, bs), 4.56 (2H, s), 6.87 (1H, d), 7.04(2H, d), 7.33 (2H, d), 7.69 (1H, d), 8.06 (1H, s).

3) The Preparation of 5-(chloromethyl)-2-(4-chlorophenoxy)pyridine

To a solution of 23.5 g (0.1 mol)(6-(4-chlorophenoxy)pyridin-3-yl)methanol in 350 mL dichloromethane wasdropwise added 17.9 g (0.15 mol) sulfoxide chloride at 0° C. then thereaction mixture was stirred for 4 hours at room temperature, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the excessive sulfoxide chloride was evaporated and the residualwas poured into water, extracted with ethyl acetate, the organic phasewas washed with water, saturated sodium bicarbonate solution, andsaturated brine successively, dried, filtered and evaporated underreduced pressure, to obtain 22.8 g target intermediate as white solid,m.p. 78-80° C. ¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃)δ(ppm): 4.55 (2H, s), 6.94 (1H, d), 7.09 (2H, d), 7.36 (2H, d), 7.75(1H, d), 8.15 (1H, s).

4) The Preparation of 2-(6-(4-chlorophenoxy)pyridin-3-yl)acetonitrile

To a solution of 2.69 g (55 mmol) sodium cyanide dissolved in 300 mLdimethyl sulfoxide was added 13.9 g (50 mmol)5-(chloromethyl)-2-(4-chlorophenoxy)pyridine and the catalytic amount of18-Crown-6 at 40° C. then the reaction mixture was raised to 80° C. toreact for 2 hours, and monitored by TLC (Thin-Layer Chromatography)until the reaction was over, the residual was poured into water,extracted with toluene, the organic phase was washed with water, andsaturated brine successively, dried, filtered and evaporated underreduced pressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:3, as aneluent) to obtain 11.2 g target intermediate as white solid, m.p.100-102° C. ¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ(ppm): 3.70 (2H, s), 6.97 (1H, d), 7.08 (2H, d), 7.37 (2H, d), 7.71 (1H,d), 8.10 (1H, s).

5) The Preparation of 2-(6-(4-chlorophenoxy)pyridin-3-yl)ethanamine

To a solution of 2-(6-(4-chlorophenoxy)pyridin-3-yl)acetonitrile 2.44 g(0.01 mol), Raney nickel (1.0 g) and 10 mL of 25% aqueous ammonia in 50mL ethanol was filled with hydrogen, then the reaction mixture wascontinued stirring at room temperature for 3-15 hours and monitored byTLC until the reaction was over, Raney nickel was filtered, the solutionwas concentrated under reduced pressure to give 2.30 g jade-green stickyliquid with yield of 95.0%, colourless oil. ¹H-NMR (300 MHz, internalstandard TMS, solvent CDCl₃) δ(ppm): 1.46 (2H, bs), 2.70 (2H, t), 2.94(2H, t), 6.87 (1H, d), 7.07 (2H, dd), 7.34 (2H, dd), 7.55 (1H, dd), 8.02(1H, d).

Example 28: The Preparation of Compound III-7

To a solution of 0.25 g (1.0 mmol)2-(6-(4-chlorophenoxy)pyridin-3-yl)ethanamine and 0.21 g (1.5 mmol)potassium carbonate in 10 mL N,N-dimethylformamide was added 0.16 g (1.0mmol) 4,5-dichloro-6-methylpyrimidine, then the reaction mixture wasraised to 80° C. to react for 2 hours, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the residual was pouredinto water, extracted with ethyl acetate, the organic phase was washedwith water, and saturated brine successively, dried, filtered andevaporated under reduced pressure, the residual was purified via silicacolumn (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 0.28 g compound III-7 as colourlessoil. ¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm):2.46 (3H, t), 2.91 (2H, t), 3.75 (2H, m), 5.43 (1H, bs), 6.89 (1H, d),7.07 (2H, d), 7.35 (2H, d), 7.58 (1H, dd), 8.03 (1H, d), 8.39 (1H, s).

Example 29: The Preparation of Compound III-202

To a solution of 0.28 g (1.0 mmol)2-(6-(4-(trifluoromethyl)phenoxy)pyridin-3-yl)ethanamine (thepreparation refers to Example 27, the difference is replacing4-chlorophenol to 4-(trifluoromethyl)phenol) and 0.21 g (1.5 mmol)potassium carbonate in 10 mL N,N-dimethylformamide was added 0.18 g (1.0mmol) 4,5-dichloro-6-ethylpyrimidine (the preparation refers to Example1, the difference is replacing ethyl 2-chloro-3-oxobutanoate to ethyl2-chloro-3-oxopentanoate). then the reaction mixture was raised to 80°C. to react for 2 hours, and monitored by TLC (Thin-LayerChromatography) until the reaction was over, the residual was pouredinto water, extracted with ethyl acetate, the organic phase was washedwith water, and saturated brine successively, dried, filtered andevaporated under reduced pressure, the residual was purified via silicacolumn (ethyl acetate/petroleum ether (boiling point range 60-90°C.)=1:4, as an eluent) to obtain 0.30 g compound III-202 as colourlessoil.

¹H-NMR (300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 1.28(3H, t), 2.78 (2H, m), 2.93 (2H, t), 3.76 (2H, m), 5.43 (1H, bs), 6.96(1H, d), 7.20-7.23 (2H, m), 7.61-7.66 (3H, m), 8.06 (1H, d), 8.44 (1H,s).

Example 30: The Preparation of Compound III-622

To a solution of 0.28 g (1.0 mmol)2-(6-(2,4-dichlorophenoxy)pyridin-3-yl)ethanamine (the preparationrefers to Example 27, the difference is replacing 4-chlorophenol to2,4-dichlorophenol) and 0.21 g (1.5 mmol) potassium carbonate in 10 mLN,N-dimethylformamide was added4,5-dichloro-6-(difluoromethyl)pyrimidine 0.20 g (1.0 mmol). then thereaction mixture was raised to 80° C. to react for 2 hours, andmonitored by TLC (Thin-Layer Chromatography) until the reaction wasover, the residual was poured into water, extracted with ethyl acetate,the organic phase was washed with water, and saturated brinesuccessively, dried, filtered and evaporated under reduced pressure, theresidual was purified via silica column (ethyl acetate/petroleum ether(boiling point range 60-90° C.)=1:4, as an eluent) to obtain 0.32 gcompound III-622 as colourless oil. ¹H-NMR (300 MHz, internal standardTMS, solvent CDCl₃) δ (ppm): 2.92 (2H, t), 3.80 (2H, m), 5.72 (1H, bs),6.54, 6.72, 6.90 (1H, t), 6.89 (1H, s), 6.98 (1H, d), 7.14 (1H, d),7.27-7.31 (2H, m), 7.48 (1H, d), 7.61 (1H, dd), 7.98 (1H, d), 8.56 (1H,s).

Example 31: The Preparation of Compound III-2630

To a solution of 0.26 g (1.0 mmol)2-(6-(4-chloro-2-methylphenoxy)pyridin-3-yl)ethanamine (the preparationrefers to Example 27, the difference is replacing 4-chlorophenol to4-chloro-2-methylphenol) and 0.21 g (1.5 mmol) potassium carbonate in 10mL N,N-dimethylformamide was added 0.18 g (1.0 mmol)4,5,6-trichloropyrimidine (the preparation refers to Example 1, thedifference is replacing ethyl 2-chloro-3-oxobutanoate to diethyl2-chloromalonate). then the reaction mixture was raised to 80° C. toreact for 2 hours, and monitored by TLC (Thin-Layer Chromatography)until the reaction was over, the residual was poured into water,extracted with ethyl acetate, the organic phase was washed with water,and saturated brine successively, dried, filtered and evaporated underreduced pressure, the residual was purified via silica column (ethylacetate/petroleum ether (boiling point range 60-90° C.)=1:4, as aneluent) to obtain 0.32 g compound III-2630 as colourless oil. ¹H-NMR(300 MHz, internal standard TMS, solvent CDCl₃) δ (ppm): 2.15 (3H, s),2.89 (2H, t), 3.73-3.79 (2H, m), 5.62 (1H, bs), 6.87 (1H, d), 6.98 (1H,d), 7.18-7.22 (2H, m), 7.54 (1H, dd), 8.00 (1H, d), 8.29 (1H, s).

Other compounds represented by the general formula PY of the presentinvention were prepared according to the above examples.

Physical properties and ¹HNMR spectrum (¹HNMR, 300 MHz, internalstandard: TMS, ppm) of some compounds of this invention are as follows:

Compound I-23: m.p. 147.5° C. δppm 2.46 (3H, s), 2.97 (2H, t), 3.78 (2H,q), 5.42 (1H, m), 7.01 (1H, d), 7.10 (2H, d), 7.30 (2H, d), 7.92 (1H,d), 8.40 (1H, s), 8.47 (1H, s).

Compound I-34: m.p. 109.0° C. δppm 2.46 (3H, s), 2.96 (2H, t), 3.79 (2H,q), 3.92 (3H, s), 5.43 (1H, m), 6.94 (1H, d), 7.12 (2H, d), 7.28 (2H,d), 8.28 (1H, d), 8.40 (1H, s), 8.82 (1H, s).

Compound I-35: yellow oil. δppm 1.38 (3H, t), 2.46 (3H, s), 2.96 (2H,t), 3.79 (2H, q), 4.38 (2H, q), 5.43 (1H, m), 6.93 (1H, d), 7.12 (2H,d), 7.28 (2H, d), 8.28 (1H, d), 8.40 (1H, s), 8.83 (1H, s).

Compound I-80: δppm 2.47 (3H, s), 2.95 (2H, t), 3.79 (2H, q), 5.55 (1H,m), 7.09 (1H, d), 7.18 (2H, m), 7.37 (1H, s), 7.93 (1H, m), 8.41 (2H,m).

Compound I-196: δppm 2.46 (3H, t), 2.96 (2H, t), 3.75 (3H, s), 3.80 (2H,dd), 5.49 (1H, t), 6.87 (2H, s), 7.02 (1H, d), 7.09 (1H, d), 7.88 (1H,d), 8.41 (2H, s).

Compound I-255: yellow oil. δppm 1.27 (3H, t), 2.79 (2H, q), 2.97 (2H,t), 3.80 (2H, q), 5.48 (1H, m), 7.02 (1H, d), 7.10 (2H, d), 7.30 (2H,d), 7.92 (1H, d), 8.46 (1H, s), 8.47 (1H, s).

Compound I-266: m.p. 102.2° C. δppm 1.26 (3H, t), 2.79 (2H, q), 2.97(2H, t), 3.79 (2H, q), 3.92 (3H, s), 5.44 (1H, m), 6.94 (1H, d), 7.12(2H, d), 8.29 (2H, d), 8.27 (1H, d), 8.45 (1H, s), 8.82 (1H, s).

Compound I-267: yellow oil. δppm 1.26 (3H, t), 1.38 (3H, t), 2.79 (2H,t), 2.98 (2H, t), 3.79 (2H, q), 4.38 (2H, q), 5.43 (1H, m), 6.93 (1H,d), 7.12 (2H, d), 7.29 (2H, d), 8.27 (1H, d), 8.45 (1H, s), 8.83 (1H,s).

Compound I-312: δppm 1.27 (3H, t), 2.80 (3H, q), 2.96 (2H, t), 3.80 (2H,q), 5.51 (1H, m), 7.09 (1H, d), 7.18 (2H, m), 7.37 (1H, s), 7.93 (1H,m), 8.40 (1H, s), 8.46 (1H, s).

Compound I-428: δppm 1.26 (3H, t), 2.79 (2H, dd), 2.96 (2H, t), 3.75(3H, s), 3.81 (2H, dd), 5.50 (1H, t), 6.87 (2H, d), 7.02 (1H, d), 7.10(1H, d), 7.88 (1H, s), 8.40 (1H, s), 8.45 (1H, s).

Compound I-467: m.p. 102-103° C. δppm 2.46 (3H, s), 2.96 (2H, t), 3.78(2H, q), 5.43 (1H, s), 7.11 (2H, d), 7.27 (2H, d), 7.78 (1H, s), 7.97(1H, s), 8.40 (1H, s).

Compound I-486: m.p. 92-93° C. δppm 2.47 (3H, s), 2.98 (2H, t), 3.80(2H, q), 5.44 (1H, s), 7.13 (2H, d), 7.30 (2H, d), 7.98 (1H, s), 8.28(1H, s), 8.41 (1H, s).

Compound I-502: m.p. 128.5° C. δppm 2.49 (3H, s), 2.89 (2H, t), 3.63(2H, q), 5.34 (1H, m), 7.06 (2H, d), 7.28 (2H, d), 7.72 (2H, s), 8.24(1H, s), 8.38 (1H, s), 8.46 (1H, s).

Compound I-602: colourless oil. Δppm 2.88 (2H, t), 4.06 (2H, q), 5.49(s, 1H), 7.21 (4H, m,), 8.28 (1H, d), 8.28 (1H, s), 68.450 (1H, s).

Compound I-618: m.p. 168.9° C. δppm 1.26 (3H, t), 2.79 (2H, q), 2.97(2H, t), 3.80 (2H, q), 5.47 (1H, m), 5.83 (2H, s), 7.13 (2H, d), 7.30(2H, d), 8.28 (1H, s), 8.40 (1H, s), 8.44 (1H, s).

Compound I-699: m.p. 146-147° C. δppm 2.45 (3H, s), 2.96 (2H, t), 3.78(2H, q), 5.45 (1H, s), 7.11 (2H, d), 7.28 (2H, d), 7.84 (1H, s), 8.41(1H, s).

Compound I-815: m.p. 98-100° C. δppm 1.26 (3H, t), 2.79 (2H, q), 2.96(2H, t), 3.79 (2H, q), 5.43 (1H, s), 7.11 (2H, d), 7.27 (2H, d), 7.84(1H, s), 8.46 (1H, s).

Compound I-929: yellow oil. δppm 2.46 (3H, s), 2.96 (2H, t), 3.87 (2H,q), 5.47 (1H, m), 7.09 (1H, m), 7.14 (2H, d), 7.28 (2H, d), 7.98 (1H,d), 8.29 (1H, d), 8.40 (1H, s).

Compound I-987: yellow oil. δppm 1.26 (3H, t), 2.79 (2H, q), 2.96 (2H,t), 3.78 (2H, q), 5.46 (1H, m), 7.13 (1H, q), 7.15 (2H, d), 7.29 (2H,d), 8.00 (1H, d), 8.30 (1H, d), 8.45 (1H, s).

Compound I-1045: m.p. 80-83° C. δppm 1.39 (3H, t), 2.46 (3H, s), 2.94(2H, t), 3.77 (2H, q), 5.47 (1H, s), 7.06 (1H, m), 7.12 (2H, d), 7.26(2H, d), 8.27 (1H, m), 8.40 (1H, s).

Compound I-1199: m.p. 147-149° C. δppm 2.47 (3H, s), 2.97 (2H, t), 3.06(3H, d), 3.62-3.79 (2H, q), 5.50 (1H, t), 7.12 (2H, d), 7.16 (1H, dd),7.32 (2H, d), 7.86 (1H, s), 8.20 (1H, dd), 8.41 (1H, s), 8.64 (1H, dd).

Compound I-1219: m.p. 113-114° C. δppm 1.39 (3H, t), 2.79 (3H, s), 2.95(2H, t), 3.78 (2H, q), 4.41 (2H, q), 5.49 (1H, t), 7.09 (3H, m), 7.27(2H, m), 8.26 (2H, m), 8.45 (1H, s).

Compound I-1414: δppm 2.47 (3H, s), 2.96 (2H, t), 3.80 (2H, q), 5.46(1H, m), 7.20 (2H, s), 7.37 (1H, s), 8.00 (1H, d), 8.24 (1H, d), 8.41(1H, s).

Compound I-1472: δppm 1.27 (3H, t), 2.80 (2H, q), 2.97 (2H, t), 3.80(2H, q), 5.47 (1H, m), 7.21 (2H, s), 7.37 (1H, s), 8.00 (1H, d), 8.25(1H, d), 8.46 (1H, s).

Compound I-1646: δppm 2.46 (3H, t), 2.96 (2H, t), 3.74 (3H, s), 3.81(2H, dd), 5.48 (1H, t), 6.89 (2H, t), 7.11 (1H, d), 7.96 (1H, d), 8.23(1H, t), 8.41 (1H, s).

Compound I-1704: δppm 1.26 (3H, t), 2.79 (2H, dd), 2.96 (2H, t), 3.73(3H, s), 3.79 (2H, dd), 5.48 (1H, t), 6.88 (2H, d), 7.12 (1H, d), 7.96(1H, d), 8.23 (1H, s), 8.45 (1H, s).

Compound I-1762: δppm 2.50 (3H, s), 2.96 (2H, t), 3.78 (2H, q), 5.54(1H, m), 7.01 (1H, d), 7.12 (1H, d), 7.30 (2H, d), 7.90 (1H, m), 8.41(1H, s), 8.44 (1H, s).

Compound I-1820: δppm 1.26 (3H, t), 2.81 (3H, q), 2.97 (2H, t), 3.78(2H, q), 5.55 (1H, m), 7.01 (1H, d), 7.11 (2H, d), 7.30 (2H, d), 7.90(1H, m), 8.44 (1H, s).

Compound I-1878: δppm 2.50 (3H, s), 2.97 (2H, t), 3.79 (2H, q), 5.53(1H, m), 7.14 (2H, d), 7.30 (3H, m), 7.99 (1H, s), 8.27 (1H, s), 8.40(1H, s).

Compound I-1936: δppm 1.26 (3H, t), 2.81 (3H, q), 2.97 (2H, t), 3.79(2H, q), 5.54 (1H, m), 7.13 (2H, d), 7.31 (2H, d), 7.98 (1H, m), 8.27(1H, s), 8.44 (1H, s).

Compound I-2052: δppm 1.30 (3H, t), 2.83 (2H, q), 2.95 (2H, t), 3.79(2H, q), 5.61 (1H, m), 7.09 (1H, d), 7.18 (2H, m), 7.33 (1H, s), 7.93(1H, m), 8.43 (1H, d).

Compound I-2400: δppm 2.98 (3H, t), 3.85 (2H, q), 5.77 (1H, m), 6.73(1H, m), 7.10 (1H, d), 7.19 (2H, m), 7.38 (1H, s), 7.94 (1H, m), 8.40(1H, s), 8.59 (1H, s).

Compound I-2458: δppm 2.98 (2H, t), 3.75 (3H, s), 3.87 (2H, dd), 5.77(1H, t), 6.72 (1H, t), 6.89 (2H, t), 7.03 (1H, d), 7.10 (1H, t), 7.88(1H, dd), 8.40 (1H, s), 8.59 (1H, s).

Compound I-2555: brown oil. δppm 8.576 (s, 1H, pyrimidine-H),7.965-7.972 (d, 1H, pyridine-6-H), 7.776-7.783 (d, 1H, pyridine-4-H),7.128-7.294 (dd, 4H, Ar—H), 6.726-7.100 (t, 1H, F₂C—H), 3.828-3.849 (q,2H, N—CH₂—C), 2.951-2.999 (t, 2H, C— CH₂—Ar).

Compound I-2611: m.p. 156-157° C. δppm 8.583 (s, 1H, pyrimidine-H),8.337-8.393 (m, 3H, pyridine-H), 7.164-7.322 (dd, 4H, Ar—H), 6.550-6.909(t, 1H, F₂C—H), 5.739 (s, 1H, NH), 3.816-3.883 (q, 2H, N—CH₂—C),2.968-3.015 (t, 2H, C—CH₂—Ar).

Compound I-2690: δppm 2.98 (2H, t), 3.74 (3H, s), 3.86 (2H, dd), 5.76(1H, t), 6.72 (1H, t), 6.88 (2H, d), 7.13 (1H, d), 7.96 (1H, d), 8.23(1H, s), 8.58 (1H, s).

Compound I-2787: δppm 8.575 (s, 1H, pyrimidine-H), 7.965-7.972 (d, 1H,pyridine-6-H), 7.775-7.782 (d, 1H, pyridine-4-H), 7.105-7.295 (dd, 4H,Ar—H), 5.882 (s, 1H, NH), 3.815-3.881 (q, 2H, N—CH₂—C), 2.955-3.001 (t,2H, C—CH₂—Ar).

Compound I-2843: m.p. 123-124° C. δppm 8.577 (s, 1H, pyrimidine-H),8.336-8.394 (m, 3H, pyridine-H), 7.152-7.325 (dd, 4H, Ar—H), 5.917 (s,1H, NH), 3.826-3.917 (q, 2H, N—CH₂—C), 2.972-3.020 (t, 2H, C—CH₂—Ar).

Compound I-3077: m.p. 130-132° C. δppm 2.46 (3H, s), 2.95 (2H, t), 3.77(2H, q), 5.50 (1H, s), 7.16 (3H, m), 7.27 (2H, m), 7.48 (1H, d), 8.40(1H, s).

Compound I-4121: δppm 2.50 (3H, s), 2.95 (2H, t), 3.77 (2H, q), 5.57(1H, m), 7.16 (3H, m), 7.29 (2H, m), 7.49 (1H, d), 8.40 (1H, s).

Compound I-5221: m.p. 121-124° C. δppm 1.26 (3H, t), 2.78 (2H, q), 2.95(2H, t), 3.78 (2H, m), 3.84 (6H, s), 5.44 (1H, s), 5.78 (1H, s), 7.20(4H, m), 8.45 (1H, s).

Compound I-6729: m.p. 102.8° C. δppm 2.49 (3H, s), 2.88 (2H, t), 3.81(2H, m), 7.11 (2H, d), 18 (1H, d), 7.30 (2H, d), 7.52 (1H, d), 8.17 (1H,d), 8.50 (1H, s), 8.78 (1H, s), 9.40 (1H, s).

Compound I-6731: m.p. 148.6° C. δppm 2.30 (3H, s), 2.49 (3H, s), 2.93(2H, t), 3.81 (2H, m), 7.27-7.05 (8H, m), 7.29 (2H, d), 7.51 (1H, d),8.14 (1H, d), 8.47 (1H, s), 8.77 (1H, s), 9.33 (1H, s).

Compound I-6732: m.p. 164.6° C. δppm 2.50 (3H, s), 2.94 (2H, t), 3.81(2H, m), 7.09 (2H, d), 7.18 (1H, d), 7.30 (2H, d), 8.18 (1H, d), 8.50(1H, s), 8.81 (1H, s), 9.28 (1H, s).

Compound I-6733: m.p. 113.7° C. δppm 2.35 (3H, s), 2.89 (2H, t), 3.64(2H, m), 7.09 (2H, d), 7.16 (1H, d), 7.30 (2H, d), 7.37 (1H, m), 8.15(1H, d), 8.19 (1H, s), 8.51 (1H, s).

Compound I-6734: m.p. 56.9° C. δppm 2.37 (3H, s), 2.90 (2H, t), 3.66(2H, m), 7.09 (2H, d), 7.16 (1H, d), 7.29 (2H, d), 7.49 (1H, m), 8.16(1H, d), 8.30 (1H, s), 8.50 (1H, s).

Compound I-6735: m.p.>300° C. δppm 2.35 (3H, s), 2.88 (2H, t), 3.62 (2H,m), 7.08 (2H, d), 7.15 (1H, d), 7.36 (1H, m), 8.15 (1H, d), 7.32 (2H,d), 8.20 (1H, s), 8.48 (1H, s).

Compound I-6790: δppm 1.23 (3H, t), 2.51 (3H, s), 2.74 (2H, q), 2.94(2H, t), 3.77 (2H, q), 5.40 (1H, m), 7.11 (2H, d), 7.26 (2H, d), 7.84(1H, s).

Compound I-6791: yellow oil. δppm 1.23 (3H, t), 2.50 (3H, s), 2.74 (2H,q), 2.96 (2H, t), 3.79 (2H, q), 5.39 (1H, m), 5.83 (2H, s), 7.13 (2H,d), 7.30 (2H, d), 8.26 (1H, s), 8.40 (1H, s).

Compound I-6793: m.p. 116.0° C. δppm 1.23 (3H, t), 2.51 (3H, s), 2.74(2H, q), 2.94 (2H, t), 3.77 (2H, q), 5.40 (1H, m), 7.10 (1H, m), 7.14(2H, d), 7.29 (2H, d), 8.00 (1H, d), 8.31 (1H, d).

Compound I-6795: yellow oil. δppm 1.24 (3H, t), 2.46 (3H, s), 2.74 (2H,q), 2.96 (2H, t), 3.78 (2H, q), 5.40 (1H, m), 7.01 (1H, d), 7.10 (2H,d), 7.30 (2H, d), 7.91 (1H, d), 8.47 (1H, s).

Compound I-6796: m.p. 90.8° C. δppm 1.23 (3H, t), 1.38 (3H, t), 2.51(3H, s), 2.74 (2H, q), 2.95 (2H, t), 3.78 (2H, q), 4.38 (2H, q), 5.38(1H, m), 6.93 (1H, d), 7.11 (2H, d), 7.29 (2H, d), 8.28 (1H, d), 8.83(1H, s).

Compound I-6797: yellow oil. δppm 1.23 (3H, t), 2.49 (3H, s), 2.74 (2H,q), 2.95 (2H, t), 3.78 (2H, q), 3.92 (3H, s), 5.39 (1H, m), 6.93 (1H,d), 7.11 (2H, d), 7.29 (2H, d), 8.28 (1H, d), 8.82 (1H, s).

Compound I-6806: δppm 1.24 (3H, t), 2.51 (3H, s), 2.75 (2H, q), 2.94(2H, t), 3.79 (2H, q), 5.40 (1H, m), 7.09 (1H, d), 7.17 (2H, m), 7.33(1H, s), 7.93 (1H, m), 8.41 (1H, s).

Compound II-19: δppm 2.52 (3H, s), 2.92 (2H, t), 3.75 (2H, dd), 5.43(1H, t), 6.81-7.01 (4H, m), 7.19 (2H, d), 7.28 (2H, d), 8.39 (1H, s).

Compound II-21: δppm 2.46 (3H, s), 2.92 (2H, t), 3.75 (2H, dd), 5.42(1H, t), 6.89 (1H, d), 6.92 (2H, d), 7.15-7.22 (3H, m), 7.47 (1H, d),8.39 (1H, s).

Compound II-25: δppm 2.45 (3H, s), 2.95 (2H, t), 3.70-3.83 (2H, q), 5.44(1H, t), 6.84 (2H, d), 7.00 (2H, d), 7.06 (1H, s), 7.26 (2H, d), 8.40(1H, s).

Compound II-53: m.p. 140-142° C. δppm 2.65 (3H, s), 3.13 (2H, t),3.65-3.76 (2H, q), 6.93 (1H, d), 7.17 (2H, d), 7.35 (2H, d), 8.31 (1H,d), 8.47 (1H, s), 8.62 (1H, t), 9.14 (1H, d).

Compound II-154: δppm 2.46 (3H, s), 2.95 (2H, t), 3.77 (2H, dd), 5.42(1H, t), 6.92 (1H, d), 7.00 (2H, d), 7.25 (2H, d), 7.43 (1H, d), 7.75(1H, s), 8.39 (1H, s).

Compound II-204: δppm 2.47 (3H, s), 2.96 (2H, t), 3.77 (2H, dd), 5.43(1H, t), 6.93 (1H, t), 7.02 (2H, d), 7.26 (2H, d), 7.37 (1H, dd), 7.48(1H, dd), 8.40 (1H, s).

Compound II-235: m.p. 140-142° C. δppm 1.25 (3H, s), 2.45 (3H, s), 2.86(2H, t), 3.72 (2H, q), 5.41 (1H, s), 6.79 (2H, d), 7.08 (2H, d), 8.39(2H, m).

Compound II-236: δppm 2.25 (3H, s), 2.45 (3H, s), 2.90 (2H, t),3.62-3.81 (2H, q), 5.43 (1H, t), 6.74 (2H, d), 7.14 (2H, d), 7.40 (1H,d), 7.77 (1H, d), 8.38 (1H, s).

Compound II-254: m.p. 183-185° C. δppm 2.45 (3H, s), 2.86 (2H, t),3.66-3.83 (2H, q), 5.43 (1H, t), 6.80 (2H, d), 7.08 (2H, d), 8.39 (1H,s).

Compound II-274: m.p. 130-132° C. δppm 2.929-2.953 (t, 2H), 3.744-3.765(q, 2H), 5.65 (s, 1H), 6.830-7.230 (dd, 4H), 8.392 (s, 1H).

Compound II-299: δppm 1.23 (3H, t), 2.78 (2H, dd), 2.92 (2H, t), 3.75(2H, dd), 5.44 (1H, t), 6.85 (1H, d), 6.91 (2H, d), 7.17-7.23 (3H, m),7.46 (1H, d), 8.44 (1H, s).

Compound II-432: δppm 1.26 (3H, t), 2.78 (2H, dd), 2.95 (2H, t), 3.77(2H, dd), 5.44 (1H, t), 6.92 (1H, d), 7.00 (2H, d), 7.25 (2H, d), 7.42(1H, d), 7.73 (1H, s), 8.44 (1H, s).

Compound II-443: m.p. 101.0° C. δppm 1.25 (3H, t), 2.77 (2H, dd), 2.92(2H, t), 3.74 (2H, dd), 5.42 (1H, t), 6.79 (2H, d), 7.18 (2H, d), 8.32(2H, s), 8.43 (1H, s).

Compound II-482: δppm 1.26 (3H, t), 2.78 (2H, dd), 2.98 (2H, t), 3.78(2H, dd), 5.44 (1H, t), 6.93 (1H, t), 7.08 (2H, d), 7.27 (2H, d), 7.37(1H, dd), 7.48 (1H, dd), 8.44 (1H, s).

Compound II-1687: δppm 2.46 (3H, s), 2.93 (2H, t), 3.75-3.96 (5H, m),5.43 (1H, t), 6.77-6.87 (4H, m), 6.93 (1H, d), 7.23 (2H, d), 8.40 (1H,s).

Compound II-1737: δppm 2.47 (3H, s), 2.95 (2H, t), 3.75-3.91 (5H, m),5.42 (1H, t), 6.80-7.04 (5H, m), 7.53 (2H, d), 8.41 (1H, s).

Compound II-1965: δppm 1.26 (3H, t), 2.79 (2H, dd), 2.95 (2H, t),3.72-3.95 (5H, m), 5.45 (1H, t), 6.78-6.90 (4H, m), 6.94 (1H, d), 7.24(2H, d), 8.45 (1H, s).

Compound II-2015: δppm 1.26 (3H, t), 2.79 (2H, dd), 2.95 (2H, t),3.75-3.95 (5H, m), 5.48 (1H, t), 6.80-6.88 (2H, q), 6.93 (2H, d), 7.01(1H, d), 7.53 (2H, d), 8.45 (1H, s).

Compound II-8917: m.p. 93.3° C. δppm 2.94 (2H, t), 3.81 (2H, dd), 5.70(1H, t), 6.72 (1H, t), 6.90-6.97 (3H, q), 7.16-7.23 (3H, q), 7.47 (1H,d), 8.57 (1H, s).

Compound II-8921: m.p. 106-107° C. δppm 2.945-2.992 (2H, t), 3.797-3.864(2H, q), 5.717 (1H, s), 6.549-6.848 (1H, t), 6.854-7.237 (7H, m), 8.583(1H, s).

Compound II-8965: m.p. 109-110° C. δppm 2.944-2.990 (2H, t), 3.798-3.865(2H, q), 5.717 (1H, s), 6.542-6.900 (1H, t), 7.010-7.588 (8H, m), 8.574(1H, s).

Compound II-9058: δppm 2.938-2.984 (2H, t), 3.790-3.858 (2H, q),6.545-6.903 (1H, t), 6.992-7.458 (4H, dd), 6.930-6.959 (1H, d),7.478-7.487 (1H, d), 7.952-7.960 (1H, s), 8.571 (1H, s).

Compound II-9073: m.p. 77-78° C. δppm 2.970-3.016 (2H, t), 3.812-3.878(2H, q), 5.738 (1H, s), 6.549-6.906 (1H, t), 7.061-7.319 (4H, dd),7.005-7.035 (1H, d), 7.698-7.727 (1H, d), 8.233 (1H, s), 8.575 (1H, s).

Compound

II-9170: m.p. 154-158° C. δppm 2.951-2.975 (2H, t), 3.800-3.821 (2H, q),6.714-6.874 (1H, t), 6.844-7.233 (4H, dd), 8.569 (1H, s).

Compound II-9336: m.p. 130-131° C. δppm 2.942-2.989 (2H, t), 3.799-3.866(2H, q), 6.994-7.459 (4H, dd), 6.936-6.965 (1H, d), 7.480-7.488 (1H, d),7.593-7.961 (1H, d), 8.571 (1H, s).

Compound II-9351: m.p. 128-129° C. δppm 2.975-3.021 (2H, t), 3.820-3.887(2H, q), 5.875 (1H, s), 7.066-7.322 (4H, dd), 7.009-7.039 (1H, d),7.704-7.731 (1H, d), 8.238 (1H, s), 8.580 (1H, s).

Compound II-10633: δppm 2.98 (2H, t), 3.79 (3H, t), 3.86 (2H, dd) 5.74(1H, s), 6.72 (1H, t), 6.84-7.05 (5H, m), 7.53 (2H, d), 8.58 (1H, s).

Compound III-1: colourless oil. δppm 2.50 (3H, s), 2.88 (2H, t), 3.74(2H, m), 5.45 (1H, bs), 6.87 (1H, d), 7.09-7.22 (3H, m), 7.36-7.42 (2H,m), 7.56 (1H, dd), 8.05 (1H, d), 8.38 (1H, s).

Compound III-5: colourless oil.

Compound III-6: colourless oil. δppm 2.46 (3H, s), 2.92 (2H, t), 3.75(2H, m), 5.42 (1H, bs), 6.90 (1H, d), 7.03 (1H, dd), 7.13-7.18 (2H, m),7.29 (1H, d), 7.59 (1H, dd), 8.05 (1H, d), 8.39 (1H, s).

Compound III-16: colourless oil. δppm 2.35 (3H, s), 2.52 (3H, s), 2.88(2H, t), 3.70-3.77 (2H, m), 5.42 (1H, bs), 6.85 (1H, d), 7.01 (2H, d),7.19 (2H, d), 7.53 (1H, dd), 8.03 (1H, d), 8.38 (1H, s).

Compound III-19: colourless oil. δppm 2.46 (3H, s), 2.89 (2H, t),3.70-3.77 (2H, m), 3.82 (3H, s), 5.42 (1H, bs), 6.83 (1H, d), 6.92 (2H,d), 7.06 (2H, d), 7.53 (1H, dd), 8.03 (1H, d), 8.38 (1H, s).

Compound III-21: colourless oil.

Compound III-22: colourless oil. δppm 2.46 (3H, t), 2.93 (2H, t), 3.76(2H, m), 5.43 (1H, bs), 6.95 (1H, d), 7.20-7.28 (2H, m), 7.60-7.66 (3H,m), 8.06 (1H, d), 8.39 (1H, s).

Compound III-82: colourless oil. δppm 2.46 (3H, s), 2.90 (2H, t), 3.74(2H, m), 5.42 (1H, bs), 6.97 (1H, d), 7.14 (1H, d), 7.28 (1H, d), 7.49(1H, d), 7.62 (1H, dd), 7.97 (1H, d), 8.38 (1H, s).

Compound III-83: colourless oil. δppm 2.46 (3H, s), 2.91 (2H, t), 3.75(2H, m), 5.42 (1H, bs), 6.97 (1H, d), 7.16 (1H, dd), 7.22 (1H, d), 7.40(1H, d), 7.61 (1H, dd), 7.99 (1H, d), 8.39 (1H, s).

Compound III-110: colourless oil. δppm 2.14 (3H, t), 2.46 (3H, t), 2.89(2H, t), 3.73 (2H, m), 5.42 (1H, bs), 6.86 (1H, d), 6.97 (1H, d),7.17-7.25 (2H, m), 7.56 (1H, dd), 7.99 (1H, d), 8.38 (1H, s).

Compound III-121: colourless oil.

Compound III-181: colourless oil. δppm 1.26 (3H, t), 2.78 (2H, m), 2.90(2H, t), 3.75 (2H, m), 5.45 (1H, bs), 6.87 (1H, d), 7.11-7.22 (3H, m),7.36-7.42 (2H, m), 7.56 (1H, dd), 8.05 (1H, d), 8.43 (1H, s).

Compound III-185: colourless oil. δppm 1.26 (3H, t), 2.78 (2H, m), 2.88(2H, t), 3.74 (2H, m), 5.43 (1H, bs), 6.94 (1H, d), 7.20 (2H, d),7.28-7.32 (1H, m), 7.47 (1H, d), 7.59 (1H, dd), 8.00 (1H, d), 8.43 (1H,s).

Compound III-186: colourless oil. δppm 1.26 (3H, t), 2.75-2.83 (2H, m),2.89-2.96 (2H, m), 3.72-3.79 (2H, m), 5.47 (1H, bs), 6.91 (1H, d), 7.03(1H, d), 7.13-7.19 (2H, m), 7.29-7.34 (1H, m), 7.60 (1H, dd), 8.06 (1H,s), 8.44 (1H, s).

Compound III-187: colourless oil. δppm 1.26 (3H, t), 2.79 (2H, m), 2.91(2H, t), 3.75 (2H, m), 5.43 (1H, bs), 6.89 (1H, d), 7.07 (2H, d), 7.35(2H, d), 7.58 (1H, dd), 8.03 (1H, dd), 8.43 (1H, s).

Compound III-196: colourless oil. δppm 1.23 (3H, t), 2.35 (3H, s),2.74-2.91 (5H, m), 3.70-3.77 (2H, m), 5.46 (1H, bs), 6.85 (1H, d), 6.99(2H, d), 7.19 (2H, d), 7.54 (1H, dd), 8.03 (1H, d), 8.43 (1H, s).

Compound III-199: colourless oil. δppm 1.26 (3H, t), 2.75-2.82 (2H, m),2.88 (2H, t), 3.70-3.77 (2H, m), 3.82 (3H, s), 5.42 (1H, bs), 6.83 (1H,d), 6.92 (2H, d), 7.06 (2H, d), 7.54 (1H, dd), 8.03 (1H, d), 8.43 (1H,s).

Compound III-201: colourless oil.

Compound III-262: colourless oil. δppm 1.26 (3H, t), 2.79 (2H, m), 2.90(2H, t), 3.74 (2H, m), 5.42 (1H, bs), 6.97 (1H, d), 7.14 (1H, d), 7.29(1H, d), 7.48 (1H, d), 7.61 (1H, dd), 7.97 (1H, d), 8.43 (1H, s).

Compound III-263: colourless oil. δppm 1.26 (3H, t), 2.81 (2H, m), 2.91(2H, t), 3.75 (2H, m), 5.43 (1H, bs), 6.98 (1H, d), 7.14-7.22 (2H, m),7.40 (2H, d), 7.63 (1H, dd), 7.99 (1H, s), 8.44 (1H, s).

Compound III-290: colourless oil. δppm 1.26 (3H, t), 2.14 (3H, s), 2.78(2H, m), 2.89 (2H, t), 3.74 (2H, m), 5.42 (1H, bs), 6.86 (1H, d), 6.97(1H, d), 7.19 (1H, dd), 7.25 (1H, d), 7.57 (1H, dd), 8.00 (1H, d), 8.43(1H, s).

Compound III-301: colourless oil.

Compound III-541: colourless oil. δppm 2.91 (2H, t), 3.81 (2H, m), 5.73(1H, bs), 6.54, 6.71, 6.83 (1H, t), 6.88 (1H, d), 7.09-7.18 (2H, m),7.22 (1H, t), 7.36-7.42 (2H, m), 7.56 (1H, dd), 8.07 (1H, d), 8.56 (1H,s).

Compound III-545: colourless oil. δppm 2.92 (2H, t), 3.80 (2H, m), 5.71(1H, bs), 6.53, 6.71, 6.89 (1H, t), 6.95 (1H, d), 7.18-7.32 (3H, m),7.47 (1H, d), 7.59 (1H, dd), 8.00 (1H, d), 8.56 (1H, s).

Compound III-546: colourless oil. δppm 2.94 (2H, t), 3.77-3.82 (2H, m),5.74 (1H, bs), 6.54, 6.72, 6.89 (1H, t), 6.91 (1H, d), 7.02 (1H, d),7.13-7.18 (2H, m), 7.29-7.35 (1H, m), 7.61 (1H, dd), 8.06 (1H, d), 8.61(1H, s).

Compound III-547: colourless oil. δppm 2.93 (2H, t), 3.80 (2H, m), 5.72(1H, bs), 6.53, 6.72, 6.89 (1H, t), 6.92 (1H, d), 7.07 (2H, d), 7.35(2H, d), 7.58 (1H, dd), 8.03 (1H, s), 8.56 (1H, s).

Compound III-556: colourless oil. δppm 2.35 (3H, t), 2.91 (2H, t),3.76-3.84 (2H, m), 5.73 (1H, bs), 6.54, 6.72, 6.84 (1H, t), 6.89 (1H,d), 7.01 (1H, d), 7.19 (1H, d), 7.55 (1H, dd), 8.04 (1H, d), 8.56 (1H,s).

Compound III-559: colourless oil. δppm 2.91 (2H, t), 3.76-3.81 (5H, m),5.73 (1H, bs), 6.54, 6.72, 6.84 (1H, t), 6.91 (1H, d), 6.94 (1H, dd),7.06 (1H, dd), 7.54 (1H, dd), 8.03 (1H, d), 8.56 (1H, s).

Compound III-561: colourless oil. δppm 2.95 (2H, t), 3.81 (2H, m), 5.74(1H, bs), 6.54, 6.72, 6.89 (1H, t), 6.95 (1H, d), 7.32 (1H, d), 7.39(1H, s), 7.44-7.54 (2H, m), 7.62 (1H, dd), 8.05 (1H, d), 8.57 (1H, s).

Compound III-562: colourless oil. δppm 2.95 (2H, t), 3.81 (2H, m), 5.74(1H, bs), 6.54, 6.72, 6.89 (1H, t), 6.97 (1H, d), 7.21-7.24 (2H, m),7.61-7.67 (3H, m), 8.06 (1H, d), 8.57 (1H, s).

Compound III-623: colourless oil. δppm 2.92 (2H, t), 3.80 (2H, m), 5.72(1H, bs), 6.54, 6.72, 6.89 (1H, t), 6.91 (1H, s), 6.99 (1H, d),7.15-7.22 (2H, m), 7.40 (1H, d), 7.61 (1H, dd), 8.00 (1H, d), 8.57 (1H,s).

Compound III-650: colourless oil. δppm 2.13 (3H, s), 2.91 (2H, t), 3.79(2H, m), 5.66 (1H, bs), 6.53, 6.72, 6.86 (1H, t), 6.89 (1H, s), 6.97(1H, d), 7.17-7.25 (2H, m), 7.57 (1H, dd), 8.01 (1H, d), 8.56 (1H, s).

Compound III-661: colourless oil.

Compound III-2521: colourless oil. δppm 2.90 (2H, t), 3.74-3.81 (2H, m),5.60 (1H, bs), 6.83-6.89 (1H, m), 7.09-7.11 (2H, m), 7.13-7.22 (1H, m),7.37-7.42 (2H, m), 7.49-7.56 (1H, m), 8.15 (1H, d), 8.29 (1H, s).

Compound III-2526: colourless oil. δppm 2.92 (2H, t), 3.74-3.81 (2H, m),5.62 (1H, bs), 6.91 (1H, d), 7.02 (1H, d), 7.14-7.18 (2H, m), 7.29-7.34(1H, m), 7.57-7.60 (1H, m), 8.05 (1H, d), 8.32 (1H, s).

Compound III-2527: colourless oil. δppm 2.91 (2H, t), 3.74-3.81 (2H, m),5.60 (1H, bs), 6.90 (1H, d), 7.07 (2H, dd), 7.35 (2H, dd), 7.54 (1H,dd), 8.03 (1H, d), 8.29 (1H, s).

Compound III-2536: colourless oil. δ(CDCl₃): 2.36 (3H, s), 2.89 (2H, t),3.73-3.79 (2H, m), 5.62 (1H, bs), 6.85 (1H, d), 6.98-7.02 (2H, m), 7.20(2H, d), 7.54 (1H, dd), 8.03 (1H, d), 8.29 (1H, s).

Compound III-2539: colourless oil. δppm 2.89 (2H, t), 3.73-3.79 (2H, m),3.81 (3H, t), 5.61 (1H, bs), 6.83 (1H, d), 6.92 (2H, dd), 7.05 (2H, dd),7.52 (1H, dd), 8.03 (1H, d), 8.29 (1H, s).

Compound III-2541: colourless oil. δppm 2.93 (2H, t), 3.75-3.82 (2H, m),5.62 (1H, bs), 6.94 (1H, d), 7.32 (1H, d), 7.40-7.51 (3H, m), 7.60 (1H,dd), 8.04 (1H, d), 8.30 (1H, s).

Biological Testing

The compounds of the present invention exhibit both excellent fungicidalactivity against many fungi in agricultural field and betterinsecticidal and acaricidal activities.

Except for the controls CK1-CK21 (known compounds illustrated inbackground technology) listed in following Table 303-310, according tothe prior art, the following compounds CK22-CK84, diflumetorim andflufenerim were also prepared as controls, all the controls wereself-made, they are listed in Table 302.

TABLE 302 the structure of controls No. Structure CK22

CK23

CK24

CK25

CK26

CK27

CK28

CK29

CK30

CK31

CK32

CK33

CK34

CK35

CK36

CK37

CK38

CK39

CK40

CK41

CK42

CK43

CK44

CK45

CK46

CK47

CK48

CK49

CK50

CK51

CK52

CK53

CK54

CK55

CK56

CK57

CK58

CK59

CK60

CK61

CK62

CK63

CK64

CK65

CK66

CK67

CK68

CK69

CK70

CK71

CK72

CK73

CK74

CK75

CK76

CK77

CK78

CK79

CK80

CK81

CK82

CK83

CK84

Example 32: Fungicidal Testing

(1) The Determination of Protectant Activity In Vivo

The method is as followed: The whole plant is used in this test. Thecompound is dissolved in a proper solvent to get mother solution. Theproper solvent is selected from acetone, methanol, DMF and so onaccording to their dissolving capability to the sample. The volume rateof solvent and testing solution (v/v) is equal to or less than 5%. Themother solution is diluted with water containing 0.1% tween-80 to getthe testing solution whose concentration is designed. The testingsolution is sprayed to the host plant by a special plant sprayer. Theplant is inoculated with fungus after 24 hours. According to theinfecting characteristic of fungus, the plant is stored in a humiditychamber and then transferred into greenhouse after infection isfinished. And the other plants are placed in greenhouse directly. Theactivity of compound is obtained by eyeballing after 7 days in common.

The protectant activities in vivo of some compounds are as follows:

The protectant activity against cucumber downy mildew in vivo:

At the dosage of 400 ppm, the protectant activity of compounds I-22,I-35, I-254, I-255, I-467, I-483, I-486, I-502, I-583, I-602, I-699,I-815, I-987, I-1762, I-1878, I-2555, I-2574, I-2748, I-2611, I-3077,I-3309, I-4757, I-5221, I-6730, I-6732, I-6740, I-6765, I-6790, I-6796,II-21, II-25, II-69, II-154, II-204, II-236, II-254, II-297, II-299,II-303, II-347, II-432, II-482, II-1687, II-1965, II-8915, II-8917,II-8921, II-8965, II-9058, II-10583, III-1, III-5, III-7, III-16,III-19, III-22, III-82, III-110, III-121, III-181, III-187, III-196,III-199, III-201, II-202, III-262, III-263, III-290, III-301, III-541,III-547, III-556, III-562, III-622, III-623, III-650, III-2521,III-2526, III-2527, III-2536, III-2539, III-2541, III-2630 and so on was100%, the protectant activity of compounds I-618, I-1199, I-2787,I-2843, I-6793, I-6797, II-235, II-274, II-9073, II-9170, II-9336,II-19334 and so on was between 80%-99%;

At the dosage of 100 ppm, the protectant activity of compounds I-22,I-254, I-255, I-467, I-583, I-602, I-699, I-987, I-1199, I-2748, I-3077,I-4757, I-6730, I-6732, I-6740, I-6765, II-21, II-204, II-236, II-297,II-299, II-482, II-1687, II-8915, II-8917, II-8921, II-8965, II-10583,III-1, III-5, III-7, III-16, III-19, III-22, III-82, III-110, III-121,III-181, III-187, III-196, III-199, III-201, III-202, III-262, III-263,III-301, III-541, III-547, III-556, III-562, III-622, III-623, III-650,III-2521, III-2526, III-2527, III-2536, III-2539, III-2541 and so on was100%, the protectant activity of compounds I-35, I-502, I-987, I-2555,I-2611, I-3309, I-5221, I-6790, I-6796, II-25, II-69, II-303, II-347,II-9058, III-290, III-2630 and so on was between 80%-99%;

At the dosage of 50 ppm, the protectant activity of compounds I-22,I-254, I-255, I-467, I-2748, I-3077, I-6730, I-6765, II-21, II-204,II-236, II-297, II-482, II-1687, II-8917, II-8965, III-1, III-5, III-7,III-16, III-19, III-22, III-82, III-110, III-121, III-181, III-187,III-196, III-201, III-202, III-262, III-263, III-301, III-541, III-547,III-556, III-562, III-622, III-623, III-650, III-2521, III-2526,III-2527, III-2536, III-2539, III-2541 and so on was 100%, theprotectant activity of compounds I-583, I-602, I-699, I-987, I-1199,I-2611, I-3309, I-5221, I-6790, I-6796, II-25, II-299, II-8915, II-8921,II-9058, II-10583, III-199, III-2630 and so on was between 80%-99%;

At the dosage of 25 ppm, the protectant activity of compounds I-22,I-255, I-467, I-583, I-699, I-3077, I-6730, I-6732, I-6765, II-204,II-236, II-297, II-482, II-8917, III-1, III-5, III-7, III-16, III-19,III-22, III-82, III-110, III-121, III-181, III-187, III-196, III-201,III-202, III-262, III-263, III-301, III-541, III-547, III-556, III-562,III-622, III-623, III-2521, III-2526, III-2527, III-2539 and so on was100%, the protectant activity of compounds I-602, I-699, I-3309, I-6790,II-25, II-1687, II-8915, II-8921, II-8965, II-10583, III-199, III-650,III-2536, III-2541 and so on was between 80%-99%;

At the dosage of 12.5 ppm, the protectant activity of compounds I-22,III-1, III-7, III-16, III-22, III-187, III-202, III-301, III-541,III-556, III-562, III-622, III-2521, III-2527 and so on was 100%, theprotectant activity of compounds I-255, I-3077, I-6765, II-204, II-482,II-8915, II-8917, II-10583, III-19, III-82, III-196, III-201, III-263,III-623, III-650, III-2536, III-2539 and so on was between 80%-99%;

At the dosage of 6.25 ppm, the protectant activity of compounds I-22,III-7, III-16, III-22, III-187, III-202, III-301, III-541, III-562 andso on was 100%, the protectant activity of compounds I-6765, II-8915,II-8917, II-10583, III-19, III-196, III-556, III-622 and so on wasbetween 80%-99%.

The protectant activity against wheat powdery mildew in vivo:

At the dosage of 400 ppm, the protectant activity of compounds I-22,I-23, I-34, I-35, I-254, I-255, I-266, I-267, I-467, I-486, I-502,I-602, I-815, I-929, I-987, I-1219, I-1414, I-1472, I-1762, I-2342,I-2555, I-2574, I-3309, I-4121, I-4757, I-6729, I-6730, I-6731, I-6732,I-6733, I-6734, I-6735, I-6739, I-6740, I-6741, I-6742, I-6756, I-6757,I-6758, I-6763, I-6765, I-6790, I-6793, I-6795, I-6796, II-19, II-25,II-69, II-154, II-204, II-297, II-299, II-303, II-347, II-432, II-482,II-1687, II-1965, II-8917, II-8921, II-8965, II-9058, II-9073, II-10583,II-19334, III-1, III-5, III-6, III-7, III-16, III-19, III-21, III-22,III-82, III-83, III-110, III-121, III-181, III-185, III-186, III-187,III-196, III-199, III-201, III-202, III-262, III-263, III-301, III-541,III-545, III-546, III-547, III-556, III-559, III-561, III-562, III-622,III-623, III-650, III-2536, III-2541 and so on was 100%; compoundsI-483, I-583, I-2748, I-2787, I-2922, I-3077, I-5221, I-6797, II-53,II-9351, III-2539 and so on was between 80%-99%.

At the dosage of 100 ppm, the protectant activity of compounds I-22,I-254, I-255, I-267, I-467, I-486, I-602, I-987, I-1414, I-1472, I-2342,I-2555, I-2574, I-6729, I-6730, I-6739, I-6740, I-6741, I-6742, I-6756,I-6757, I-6758, I-6763, I-6765, I-6793, II-154, II-204, II-297, II-303,II-347, II-432, II-482, II-1687, II-8921, II-8965, II-10583, II-19334,III-121, III-202, III-301 and so on was 100%; compounds I-23, I-483,I-502, I-583, I-6731, I-6732, I-6733, I-6735, II-19, II-25, II-299,II-8917, II-9058, II-9073, III-1, III-5, III-7, III-22, III-82, III-110,III-181, III-541, III-545, III-562, III-2541 and so on was between80%-99%.

At the dosage of 25 ppm, the protectant activity of compounds I-22,I-254, I-255, I-2342, I-2555, I-2574, I-6730, I-6739, I-6740, I-6742,I-6765, I-6793, II-204, II-297, II-303, II-347, II-432, II-482, II-1687,II-8921, II-10583, II-19334, III-202 and so on was 100%; compounds I-23,I-254, I-502, I-602, I-987, I-6729, I-6731, I-6732, I-6733, I-6735,I-6756, I-6763, II-19, II-299, II-8917, II-8965, II-9058, II-9073,III-121, III-301 and so on was between 80%-99%.

At the dosage of 6.25 ppm, the protectant activity of compounds I-22,I-2342, I-2574, I-6765, II-204, II-432, II-10583 and II-19334 and so onwas 100%; compounds I-23, I-255, I-502, I-2555, I-6730, I-6739, I-6742,II-19, II-297, II-303, II-482, II-1687, II-8921, III-202 and so on wasbetween 80%-99%.

The protectant activity against corn rust in vivo:

At the dosage of 400 ppm, the protectant activity of compounds I-22,I-35, I-254, I-266, I-267, I-467, I-483, I-486, I-583, I-815, I-929,I-987, I-1045, I-1199, I-1219, I-1472, I-1762, I-1878, I-2342, I-2555,I-2574, I-2922, I-3077, I-4121, I-4757, I-5221, I-6729, I-6730, I-6731,I-6732, I-6733, I-6734, I-6735, I-6739, I-6740, I-6741, I-6742, I-6756,I-6757, I-6758, I-6763, I-6765, I-6790, I-6791, I-6793, I-6795, I-6796,II-19, II-21, II-53, II-69, II-154, II-165, II-204, II-297, II-299,II-303, II-347, II-432, II-482, II-1687, II-1965, II-8915, II-8917,II-8921, II-8965, II-10583, II-19334, III-1, III-6, III-7, III-16,III-19, III-21, III-82, III-83, III-110, III-181, III-185, III-186,III-196, III-199, III-201, III-202, III-262, III-301, III-541, III-545,III-546, III-547, III-556, III-559, III-561, III-622, III-623, III-661,III-2521, III-2526, III-2536, III-2539, III-2630 and so on was 100%;compounds I-1627, I-2748, II-25, II-236, II-254, III-5, III-22, III-650,III-2527, III-2541 and so on was between 80%-99%.

At the dosage of 100 ppm, the protectant activity of compounds I-22,I-35, I-254, I-467, I-486, I-583, I-987, I-2342, I-2574, I-2922, I-4757,I-5221, I-6729, I-6731, I-6732, I-6733, I-6734, I-6735, I-6739, I-6740,I-6741, I-6742, I-6756, I-6757, I-6758, I-6763, I-6765, I-6796, II-21,II-69, II-154, II-204, II-297, II-299, II-303, II-347, II-432, II-482,II-1687, II-8915, II-8917, II-8965, II-10583, III-6, III-7, III-21,III-110, III-201, III-202, III-262, III-301, III-545, III-546, III-559,III-561, III-622, III-661 and so on was 100%; compounds I-267, I-815,I-1199, I-1219, I-3077, I-3309, I-6730, I-6791, II-19, II-165, II-8921,II-19334, III-19, III-82, III-181, III-185, III-186, III-196, III-199,III-547, III-556, III-623, III-2526 and so on was between 80%-99%.

At the dosage of 25 ppm, the protectant activity of compounds I-22,I-254, I-583, I-2342, I-6729, I-6742, II-69, II-154, II-204, II-303,II-432, II-482, II-8915, II-8917, II-8965, III-7, III-262, III-561,III-622 and so on was 100%; compounds I-35, I-266, I-467, I-987, I-1219,I-2574, I-4757, I-5221, I-6730, I-6731, I-6732, I-6733, I-6734, I-6735,I-6739, I-6740, I-6765, I-6757, I-6796, II-21, II-297, II-299, II-347,II-8921, II-10583, III-199, III-201, III-545, III-546, III-559 wasbetween 80%-99%.

At the dosage of 6.25 ppm, the protectant activity of compounds I-22,I-254, I-2342, I-6742, II-154, II-303, II-432, II-482, II-8915, II-8917and so on was 100%; compounds I-266, I-987, I-2574, I-6732, I-6733,I-6796, II-21, II-204, II-297, II-299, II-347, II-8921, II-8965,III-262, III-559, III-561, III-622 was between 80%-99%.

(2) Determination of Fungicidal Activity In Vitro

The method is as followed: High Through Put is used in the test. Thecompound is dissolved in a proper solvent to become a testing solutionwhose concentration is designed. The solvent is selected from acetone,methanol, DMF and so on according to their dissolving capability to thesample. In a no animalcule condition, the testing solution and pathogenssuspension are added into the cells of 96 cells culture board, whichthen should be placed in the constant temperature box. 24 hours later,pathogen germination or growth can be investigated by eyeballing, andthe activity in vitro of the compound is evaluated based on germinationor growth of control treatment.

The activities in vitro (inhibition rate) of some compounds are asfollows:

The inhibition rate against rice blast:

At the dosage of 25 ppm, the inhibition rate of compounds I-22, I-483,I-929, I-987, I-1762, I-2574, I-2922, I-6757, I-6758, I-6763, II-53,II-165, II-274, II-1965, III-7, III-121, III-301, III-661 and so on was100%; compounds I-23, I-35, I-254, I-255, I-266, I-618, I-1199, I-1219,I-1878, I-2342, I-3077, I-3309, I-4121, I-4757, I-5221, I-6729, I-6730,I-6731, I-6732, I-6733, I-6734, I-6735, I-6742, I-6758, I-6791, I-6793,I-6795, I-6796, I-6797, II-19, II-25, II-69, II-204, II-347, II-482,II-1687, II-9336, II-10583, III-1, III-5, III-6, III-7, III-16, III-19,III-21, III-22, III-82, III-83, III-110, III-181, III-186, III-187,III-196, III-199, III-201, III-202, III-262, III-541, III-545, III-546,III-547, III-556, III-559, III-561, III-562, III-622, III-623, III-661,III-2521, III-2526, III-2536, III-2539, III-2541, III-2630 was between80%-99%, contrast compounds CK4, CK5, CK6, CK10, CK20, CK32, CK33, CK35,CK37, CK40, CK41, CK43, CK46, CK47, CK48, CK49, CK50, CK55, CK56 andCK58 was less than 50%, contrast compounds CK1, CK2, CK3, CK7, CK11,CK13, CK15, CK16, CK21, CK38, CK39, CK44, CK45, CK59, CK60, CK61 andCK63 was all 0;

At the dosage of 8.3 ppm, the inhibition rate of compounds I-483,I-2574, I-2922, II-53, II-165, III-7, III-661 and so on was 100%;compounds I-22, I-929, I-987, I-6758 and II-274 was between 80%-99%,contrast compound CK17 was 50%; contrast compounds CK5, CK6, CK14, CK18,CK19, CK46, CK47, CK48, CK49, CK50, CK51, CK52 and diflumetorim was all0;

At the dosage of 2.8 ppm, the inhibition rate of compounds I-483,I-2922, II-53, II-165, III-7 and so on was 100%; compound II-274 wasbetween 80%-99%, contrast compound CK17 was 0;

At the dosage of 0.9 ppm, the inhibition rate of compounds I-483,I-2922, II-53, II-165, III-7 and so on was 100%;

At the dosage of 0.3 ppm, the inhibition rate of compounds I-483,I-2922, II-53, II-165 and III-7 was 100%;

At the dosage of 0.1 ppm, the inhibition rate of compounds I-483,I-2922, II-165 and III-7 was 100%;

The inhibition rate against cucumber gray mold:

At the dosage of 25 ppm, the inhibition rate of compounds I-486, I-1045,I-2342, I-4757, II-303, II-1965, II-8921, III-82 and so on was 100%;compounds I-1199, I-3309, II-69, II-347, III-7, III-199, III-202,III-262, III-545, III-547, III-559, III-622 was between 80%-99%,contrast compounds CK20, CK21, CK24, CK25, CK44, CK45, CK56, CK57, CK62was less than 50%, contrast compounds CK1, CK2, CK3, CK4, CK6, CK7, CK8,CK9, CK10, CK13, CK14, CK15, CK16, CK17, CK22, CK26, CK32, CK33, CK34,CK35, CK46, CK47, CK48, CK51, CK52, CK53, CK54, CK55, CK58, CK59, CK60,CK61, CK63, CK67, CK68, CK70, CK73, CK74, CK75, CK76, CK77, CK78, CK79,CK80, CK81, CK82, CK83, CK84, diflumetorim and flufenerim was all 0;

(2) The Contrastive Test Results of Some Compounds and Contrasts

Contrastive tests were carried out between some compounds and contrasts.The test results are listed in table 303-table 305 (“///” in thefollowing tables means no test).

TABLE 303 The comparative test of protectant activity against cucumberdowny mildew control effect against cucumber downy mildew (%) Compound400 100 50 25 12.5 6.25 3.125 No. mg/L mg/L mg/L mg/L mg/L mg/L mg/LI-22 100 100 100 100 100 100 85 I-3309 100 90 90 90 70 60 50 II-236 100100 100 100 /// /// /// II-297 100 100 100 100 /// /// /// II-8915 100100 100 99 95 90 20 II-8917 100 100 100 100 95 85 /// II-10583 100 100100 95 95 95 /// III-1 100 100 100 100 100 /// /// III-5 100 100 100 100/// /// /// III-7 100 100 100 100 100 100 100 III-16 100 100 100 100 100100 /// III-19 100 100 100 100 98 95 /// III-22 100 100 100 100 100 100/// III-82 100 100 100 100 98 /// /// III-110 100 100 100 100 /// ////// III-121 100 100 100 100 /// /// /// III-181 100 100 100 100 /// ////// III-187 100 100 100 100 100 100 /// III-196 100 100 100 100 85 85/// III-201 100 100 100 100 98 /// /// III-202 100 100 100 100 100 100/// III-262 100 100 100 100 /// /// /// III-263 100 100 100 100 98 70/// III-301 100 100 100 100 100 100 /// III-541 100 100 100 100 100 10095 III-547 100 100 100 100 /// /// /// III-556 100 100 100 100 100 95/// III-562 100 100 100 100 100 100 /// III-622 100 100 100 100 100 98/// III-623 100 100 100 100 98 70 /// III-650 100 100 100 98 95 /// ///III-2521 100 100 100 100 100 /// /// III-2527 100 100 100 100 100 75 ///III-2536 100 100 100 98 90 /// /// III-2539 100 100 100 100 85 /// ///CK1 100 100 100 100 50 30 20 CK3 80 /// /// /// /// /// /// CK6 70 ////// /// /// /// /// CK7 70 30 0 0 /// /// /// CK8 98 95 80 75 /// ////// CK9 100 98 90 70 /// /// /// CK10 100 82 40 20 /// /// /// CK11 8530 0 0 /// /// /// CK13 85 25 0 0 /// /// /// CK14 98 40 0 0 /// /// ///CK15 95 15 0 0 /// /// /// CK16 85 /// /// /// /// /// /// CK17 100 4010 0 /// /// /// CK20 100 10 0 0 /// /// /// CK22 100 98 75 60 /// ////// CK23 100 0 0 0 /// /// /// CK25 100 0 0 0 /// /// /// CK26 100 60 400 /// /// /// CK27 100 0 0 0 /// /// /// CK28 100 40 20 0 /// /// ///CK29 98 98 90 25 /// /// /// CK32 60 /// /// /// /// /// /// CK33 0 ////// /// /// /// /// CK34 85 /// /// /// /// /// /// CK35 60 /// /// ////// /// /// CK37 100 20 10 0 /// /// /// CK42 100 100 100 20 0 0 0 CK43100 40 20 0 /// /// /// CK52 100 98 90 70 /// /// /// CK53 100 90 85 60/// /// /// CK54 100 90 80 65 /// /// /// CK55 100 0 0 0 /// /// ///CK56 100 10 0 0 /// /// /// CK57 50 /// /// /// /// /// /// CK58 0 ////// /// /// /// /// CK59 80 /// /// /// /// /// /// CK60 100 10 0 0 ////// /// CK61 100 90 85 30 /// /// /// CK62 80 /// /// /// /// /// ///CK63 70 /// /// /// /// /// /// CK65 0 /// /// /// /// /// /// CK66 0/// /// /// /// /// /// CK67 100 60 20 0 /// /// /// CK68 0 /// /// ////// /// /// CK69 100 100 98 50 /// /// /// CK70 100 60 30 0 /// /// ///CK71 80 /// /// /// /// /// /// CK72 100 100 40 20 /// /// /// CK73 9898 95 60 /// /// /// CK74 50 /// /// /// /// /// /// CK75 60 /// /// ////// /// /// CK76 0 /// /// /// /// /// /// CK77 0 /// /// /// /// ////// CK78 0 /// /// /// /// /// /// CK79 85 /// /// /// /// /// /// CK8085 /// /// /// /// /// /// CK83 100 100 98 85 /// /// /// CK84 100 100100 85 /// /// /// diflumetorim 100 100 100 70 15 0 /// flufenerim 0 ////// /// /// /// ///

TABLE 304 The comparative test of protectant activity against wheatpowdery mildew control effect against wheat powdery mildew (%) Compound400 100 25 6.25 1.6 0.4 No. mg/L mg/L mg/L mg/L mg/L mg/L I-22 100 100100 100 15 /// I-254 100 100 100 100 20 /// I-2342 100 100 100 100 95 60I-2574 100 100 100 100 75 20 I-6765 100 100 100 100 /// /// II-204 100100 100 100 /// /// II-297 100 100 100 90 40 30 II-303 100 100 100 90 8025 II-432 100 100 100 100 80 50 II-482 100 100 100 98 /// /// II-8921100 100 100 90 40 /// II-10583 100 100 100 100 /// /// II-19334 100 100100 100 60 /// III-1 100 98 98 98 /// /// III-202 100 100 100 95 /// ///CK1 100 100 100 80 /// /// CK2 100 100 80 0 /// /// CK4 40 0 /// /// ////// CK6 100 100 90 85 0 0 CK8 0 /// /// /// /// /// CK9 100 0 0 0 ////// CK10 50 /// /// /// /// /// CK11 100 60 40 0 /// /// CK12 80 30 0 0/// /// CK13 40 0 0 0 /// /// CK14 85 10 0 0 /// /// CK15 95 85 10 0 ////// CK16 70 /// /// /// /// /// CK17 100 75 70 50 /// /// CK19 50 0 ////// /// /// CK20 100 30 0 0 /// /// CK21 0 /// /// /// /// /// CK22 10090 50 0 /// /// CK23 100 0 0 0 /// /// CK24 0 0 /// /// /// /// CK25 0/// /// /// /// /// CK26 70 /// /// /// /// /// CK27 80 /// /// /// ////// CK29 100 80 50 40 /// /// CK30 100 80 20 0 /// /// CK31 0 0 0 0 ////// CK32 0 /// /// /// /// /// CK33 0 /// /// /// /// /// CK34 0 /// ////// /// /// CK35 0 /// /// /// /// /// CK36 100 80 60 0 /// /// CK37 0/// /// /// /// /// CK41 100 70 50 0 /// /// CK42 100 70 60 50 /// ///CK43 20 /// /// /// /// /// CK44 0 /// /// /// /// /// CK45 0 /// ////// /// /// CK48 30 0 0 0 /// /// CK51 100 80 40 0 /// /// CK53 100 80 00 /// /// CK52 0 /// /// /// /// /// CK55 60 /// /// /// /// /// CK56 70/// /// /// /// /// CK57 0 /// /// /// /// /// CK58 0 /// /// /// ////// CK59 0 /// /// /// /// /// CK60 0 /// /// /// /// /// CK61 70 ////// /// /// /// CK63 50 /// /// /// /// /// CK65 0 /// /// /// /// ///CK66 0 /// /// /// /// /// CK67 0 /// /// /// /// /// CK68 0 /// /// ////// /// CK69 100 0 0 0 /// /// CK70 98 0 0 0 /// /// CK71 100 /// ////// /// /// CK72 100 70 60 50 /// /// CK73 40 /// /// /// /// /// CK74 0/// /// /// /// /// CK75 0 /// /// /// /// /// CK76 75 /// /// /// ////// CK77 100 100 80 70 /// /// CK78 0 /// /// /// /// /// CK79 0 /// ////// /// /// CK80 100 80 0 0 /// /// CK81 40 /// /// /// /// /// CK82 10080 0 0 /// /// CK83 100 100 70 40 /// /// diflumetorim 100 95 95 90 //////

TABLE 305 The comparative test of protectant activity against corn rustcontrol effect against corn rust (%) Compound 400 100 25 6.25 1.6 0.4No. mg/L mg/L mg/L mg/L mg/L mg/L I-22 100 100 100 100 50 20 I-254 100100 100 100 95 40 II-154 100 100 100 100 50 /// II-303 100 100 100 10080 50 II-432 100 100 100 100 75 15 II-482 100 100 100 100 /// ///II-8915 100 100 100 100 80 30 II-8917 100 100 100 100 60 10 II-8965 100100 100 95 85 30 III-7 100 100 100 /// /// /// III-262 100 100 100 90 9060 III-561 100 100 100 95 80 40 CK2 100 100 100 85 /// /// CK4 0 0 ////// /// /// CK5 95 98 40 30 /// /// CK6 100 100 100 80 30 0 CK8 50 ////// /// /// /// CK9 100 100 20 0 /// /// CK10 50 /// /// /// /// ///CK12 100 100 85 75 /// /// CK13 100 0 0 0 /// /// CK14 100 20 0 0 ////// CK15 95 85 30 0 /// /// CK16 0 /// /// /// /// /// CK17 100 0 0 0//// /// CK18 80 30 0 /// /// /// CK19 70 0 /// /// /// /// CK20 100 700 0 /// /// CK21 85 /// /// /// /// /// CK22 100 100 40 0 /// /// CK23100 0 0 0 /// /// CK24 100 50 20 0 /// /// CK25 0 /// /// /// /// ///CK26 100 0 0 0 /// /// CK27 100 100 90 30 /// /// CK28 100 100 100 95 00 CK29 100 95 85 30 /// /// CK30 0 0 0 0 /// /// CK31 0 0 0 0 /// ///CK33 0 /// /// /// /// /// CK34 0 /// /// /// /// /// CK35 0 /// /// ////// /// CK36 100 60 40 0 /// /// CK37 0 /// /// /// /// /// CK38 0 ////// /// /// /// CK39 100 100 80 50 10 0 CK40 100 100 90 70 30 0 CK41 100100 90 80 20 0 CK42 70 /// /// /// /// /// CK43 85 /// /// /// /// ///CK44 85 /// /// /// /// /// CK45 80 /// /// /// /// /// CK46 40 0 0 0/// /// CK47 80 30 0 0 /// /// CK48 60 20 0 0 /// /// CK49 85 30 0 0 ////// CK50 80 0 0 0 /// /// CK51 80 20 0 0 /// /// CK52 85 /// /// /// ////// CK53 0 /// /// /// /// /// CK54 100 60 30 0 /// /// CK55 0 /// ////// /// /// CK56 70 /// /// /// /// /// CK57 0 /// /// /// /// /// CK580 /// /// /// /// /// CK59 0 /// /// /// /// /// CK60 0 /// /// /// ////// CK61 0 /// /// /// /// /// CK63 100 30 0 0 /// /// CK65 0 /// ////// /// /// CK66 0 /// /// /// /// /// CK67 0 /// /// /// /// /// CK68 0/// /// /// /// /// CK69 100 90 50 0 /// /// CK70 100 30 10 0 /// ///CK71 0 /// /// /// /// /// CK72 100 80 20 0 /// /// CK73 100 90 10 0 ////// CK74 100 100 90 85 /// /// CK75 0 /// /// /// /// /// CK76 70 ////// /// /// /// CK77 100 60 40 0 /// /// CK78 0 /// /// /// /// /// CK790 /// /// /// /// /// CK80 100 85 20 0 /// /// CK81 80 /// /// /// ////// CK82 100 30 0 0 /// /// CK83 30 /// /// /// /// /// CK84 100 90 60 0/// /// diflumetorim 100 80 10 0 /// ///

Example 33: Bioactivity Test Against Insects and Mites

Determination of insecticidal activity of compounds of the presentinvention against a few insects were carried out by the followingprocedures:

Compounds were dissolved in mixed solvent (acetone:methanol=1:1), anddiluted to required concentration with water containing 0.1% of tween80.

Diamond back moth, armyworm, peach aphid and carmine spider mite wereused as targets and the method of spraying by airbrush was used fordetermination of insecticidal biassays.

(1) Bioactivity Test Against Diamond Back Moth

(1) Determination of Insecticidal Activity Against Diamond Back Moth

The method of spraying by airbrush: The cabbage leaves were made intoplates of 2 cm diameter by use of punch. A test solution (0.5 ml) wassprayed by airbrush at the pressure of 0.7 kg/cm² to both sides of everyplate. 10 Second instar larvae were put into the petri-dishes after theleaf disc air-dried and 3 replicates were set for each treatment. Thenthe insects were maintained in observation room (25° C., 60˜70% R.H.).Scores were conducted and mortalities were calculated after 72 hrs.

Part of Test Results Against Diamond Back Moth:

At the dosage of 600 ppm, compounds I-22, I-254, I-255, I-467, I-583,I-815, I-3077, I-3309, I-4121, I-6729, I-6731, I-6732, I-6733, I-6734,I-6735, I-6739, I-6740, I-6742, I-6756, I-6757, I-6758, I-6765, II-19,II-154, II-204, II-297, II-347, II-482, II-1687, II-1965, II-8915,II-8965, II-10583, II-19334, III-1, III-6, III-7, III-16, III-19,III-21, III-22, III-110, III-181, III-185, III-187, III-196, III-199,III-201, III-202, III-541, III-546, III-547, II-556, III-559, III-562,III-622 and III-2527 showed 100% control against carmine spider mite;compounds II-21, II-274, II-303, II-432, II-8917, II-9170, III-83,III-262, III-545, II-561, III-2526 and III-2539 showed 80%-99% control.

At the dosage of 100 ppm, compounds I-254, I-255, I-6739, I-6740,I-6742, I-6756, I-6757, I-6758, I-6765, I-3309, II-19, II-204, II-482,II-19334, III-196, III-546, III-547 and III-556 showed 100% controlagainst carmine spider mite; compounds II-1965, II-8965, II-9170, III-7,III-22, III-187 and III-202 showed 80%-99% control.

(2) Bioactivity Test Against Armyworm

The method of spraying by airbrush: The corn leaves were made intoplates of 2 cm diameter by use of punch. A test solution (0.5 ml) wassprayed by airbrush at the pressure of 0.7 kg/cm² to both sides of everyplate. 10 Second instar larvae were put into the petri-dishes after theleaf disc air-dried and 3 replicates were set for each treatment. Thenthe insects were maintained in observation room (25□, 60˜70% R.H.).Scores were conducted and mortalities were calculated after 72 h.

Part of Test Results Against Armyworm:

At the dosage of 600 ppm, compounds I-255, I-467, I-486, I-583, I-1472,I-2342, I-3309, I-4121, I-6729, I-6731, I-6732, I-6733, I-6734, I-6735,I-6739, I-6740, I-6741, I-6756, I-6757, I-6758, I-6763, I-6765, II-19,II-21, II-69, II-204, II-297, II-299, II-347, II-482, II-1965, II-8915,II-8917, II-8965, II-10583, II-19334, III-1, III-6, III-7, III-16,III-19, III-21, III-22, III-181, III-187, III-196, III-199, III-201,III-202, III-541, III-546, III-547, III-556, II-559, III-561, III-562and III-2527 showed 100% control against carmine spider mite; compoundsI-254, I-1762, I-2748, I-6742, II-303, II-432, III-110, III-650 andIII-2541 showed 80%-99% control.

At the dosage of 100 ppm, compounds I-255, I-3309, I-6739, I-6740,I-6741, I-6756, I-6757, I-6758, I-6763, I-6765, II-204, II-482, II-8965,III-22, III-187, III-199, III-202, III-547, III-559, III-561 and III-562showed 100% control against carmine spider mite; compounds I-1472,II-69, II-297, II-1965, II-8915, II-19334, III-196, III-201 and III-650showed 80%-99% control.

At the dosage of 10 ppm, compounds II-482, III-187, III-547 and III-562showed 80%-99% control.

(3) Bioactivity Test Against Green Peach Aphid

Method: Filter papers were put in culture dishes (Diameter=6 cm), andwater was dripped on filter papers for preserving moisture. Green peachaphids (Myzus Persicae Sulzer) were maintained on cabbage. Leaves(Diameter=3 cm) of approximately 15-30 aphids were put in the culturedishes. Bioactivity tests were used the method of Airbrush Foliar Spray,pressure=10 psi (0.7 kg/cm2), spray volume=0.5 mL. The studies wereconducted at three constant temperatures 25±1 C in incubator cabinetswith 60±5% RH. Survey the survival aphids after 48 hrs and calculate thedeath rates.

Part of Test Results Against Green Peach Aphid:

At the dosage of 600 ppm, compounds I-22, I-23, I-34, I-35, I-254,I-255, I-266, I-267, I-467, I-483, I-486, I-502, I-583, I-602, I-815,I-929, I-987, I-1414, I-1472, I-1762, I-1878, I-2342, I-2555, I-2748,I-3077, I-3309, I-4121, I-6729, I-6730, I-6731, I-6732, I-6733, I-6734,I-6735, I-6739, I-6740, I-6741, I-6742, I-6756, I-6757, I-6758, I-6763,I-6765, I-6790, I-6793, I-6795, I-6796, I-6797, II-19, II-21, II-25,II-69, II-154, II-204, II-236, II-297, II-299, II-303, II-347, II-432,II-443, II-482, II-1687, II-1965, II-8915, II-8917, II-8921, II-8965,II-9073, II-10583, II-19334, III-1, III-5, III-6, III-7, III-16, III-19,III-21, III-22, III-82, III-83, III-110, III-121, III-181, III-185,III-186, III-187, III-196, III-199, III-201, III-202, III-262, III-263,III-301, III-541, III-545, III-546, III-547, III-556, III-559, III-561,III-562, III-622, III-623, III-650, III-661, III-2527, III-2536 andIII-2539 showed 100% control against carmine spider mite; compoundsI-699, I-1199, I-5221, III-2526 and III-2541 showed 80%-99% control.

At the dosage of 100 ppm, compounds I-22, I-23, I-34, I-35, I-254,I-255, I-266, I-267, I-483, I-486, I-583, I-602, I-815, I-987, I-1414,I-1472, I-1762, I-1878, I-2342, I-2555, I-3077, I-3309, I-4121, I-6729,I-6731, I-6732, I-6733, I-6734, I-6735, I-6739, I-6740, I-6741, I-6742,I-6756, I-6757, I-6758, I-6763, I-6765, I-6793, I-6796, I-6797, II-19,II-69, II-154, II-204, II-297, II-299, II-303, II-347, II-432, II-443,II-482, II-1687, II-1965, II-8915, II-8917, II-8965, II-10583, II-19334,III-7, III-16, III-22, III-110, III-121, III-181, III-185, III-186,III-187, III-196, III-199, III-201, III-202, III-262, III-301, III-541,III-547, III-556, III-559, III-561, III-562, III-650 and III-661 showed100% control against carmine spider mite; compounds I-467, I-5221,II-21, II-25, II-8921, II-9073, III-1, III-5, III-6, III-21, III-545 andIII-546 showed 80%-99% control.

At the dosage of 10 ppm, compounds I-22, I-34, I-35, I-254, I-255,I-266, I-267, I-987, I-1472, I-1762, I-1878, I-2342, I-3309, I-4121,I-6729, I-6731, I-6732, I-6733, I-6734, I-6735, I-6739, I-6740, I-6741,I-6742, I-6756, I-6757, I-6758, I-6763, I-6765, I-6796, II-19, II-69,II-204, II-297, II-347, II-482, II-1687, II-1965, II-8915, II-8917,II-8965, II-10583, II-19334, III-22, III-181, III-187, III-202, III-301,III-547 and III-562 showed 100% control against carmine spider mite;compounds I-23, I-583, I-602, I-3077, I-6793, I-6797, II-21, II-299,III-7, III-186, III-196 and III-541 showed 80%-99% control.

At the dosage of 5 ppm, compounds I-254, I-1762, I-6731, I-6735, I-6739,I-6740, I-6741, I-6742, I-6756, I-6757, I-6758, I-6763, I-6765, II-69,II-204, II-297, II-347, II-482 and II-8915 showed 100% control againstcarmine spider mite; compounds II-299, II-8917, II-8965 and II-19334showed 80%-99% control.

At the dosage of 2.5 ppm, compounds I-254, I-6739, I-6756, I-6757,I-6758, I-6765, II-297, II-347, II-482 and II-8915 showed 100% controlagainst carmine spider mite; compounds II-69, II-204 and II-19334 showed80%-99% control.

(4) Bioactivity Test Against Carmine Spider Mite

The method: Broadbean shoots with two true leaves in pot were taken, thehealthy adults of carmine spider mite were inoculated to the leaves. Theadults were counted and then sprayed with airbrush at the pressure of0.7 kg/cm² and at dose of 0.5 ml. 3 replicates were set for eachtreatment. And then they were maintained in standard observation room.Scores were conducted and mortalities were calculated after 72 hrs.

Parts of the Test Results Against Carmine Spider Mite are as Follows:

At the dosage of 600 ppm, compounds I-22, I-23, I-254, I-255, I-266,I-267, I-483, I-583, I-602, I-929, I-987, I-1472, I-1762, I-2342,I-6729, I-6730, I-6731, I-6732, I-6733, I-6734, I-6735, I-6739, I-6740,I-6741, I-6742, I-6756, I-6757, I-6758, I-6763, I-6765, I-6795, I-6797,II-19, II-21, II-69, II-154, II-204, II-297, II-299, II-303, II-347,II-432, II-443, II-482, II-1687, II-1965, II-8915, II-8917, II-8965,II-10583, II-19334, III-1, III-5, III-7, III-16, III-19, III-21, III-22,III-110, III-181, III-185, III-187, III-196, III-199, III-201, III-202,III-541, III-545, III-547, III-556, III-559, III-561, III-562 andIII-2539 showed 100% control against carmine spider mite; compoundsI-1414, I-2555, I-3077, I-3309, I-6796, II-165, III-83, III-546 andIII-623 showed 80%-99% control.

At the dosage of 100 ppm, compounds I-22, I-254, I-255, I-266, I-987,I-1762, I-2342, I-6729, I-6731, I-6732, I-6733, I-6734, I-6735, I-6739,I-6740, I-6741, I-6756, I-6757, I-6758, I-6763, I-6765, I-6795, I-6797,II-19, II-21, II-69, II-154, II-204, II-297, II-299, II-347, II-432,II-443, II-482, II-1965, II-8915, II-8917, II-8965, II-19334, III-7,III-16, III-22, III-181, III-187, III-199, III-202, III-547, III-556,III-559 and III-562 showed 100% control against carmine spider mite;compounds I-23, I-483, I-602, I-3309, III-1, III-19, III-196, III-541and III-2539 showed 80%-99% control.

At the dosage of 10 ppm, compounds I-254, I-6739, I-6756, I-6765,II-204, II-347, II-482, II-8965 and II-19334 showed 100% control againstcarmine spider mite; compounds I-6740, I-6741, I-6757, I-6758, II-69,II-443, III-199 and III-562 showed 80%-99% control.

At the dosage of 5 ppm, compounds II-482 and II-19334 showed 100%control against carmine spider mite; compounds II-204, II-347 andII-8965 showed 80%-99% control.

At the dosage of 2.5 ppm, compounds II-482, II-8965 and II-19334 showed80%-99% control.

(5) The Contrastive Test Results of Some Compounds and Contrasts

Contrastive tests were carried out between some compounds and contrasts.The test results are listed in table 306 to table 310 (“///” in thefollowing tables means no test).

TABLE 306 contrastive tests against diamond back moth Insecticidalactivity against diamond back moth (%) Compound No. 600 mg/L 100 mg/L 10mg/L I-255 100 100 43 I-3309 100 100 60 I-6733 100 68 40 I-6734 100 5240 I-6742 100 75 47 II-19 100 100 50 II-204 100 100 20 II-347 100 70 65II-482 100 100 60 II-8965 100 80 40 III-196 100 100 /// III-546 100 100/// III-547 100 100 57 III-556 100 100 77 CK4 0 /// /// CK6 86 16 0 CK785 16 0 CK8 33 /// /// CK9 100 45 25 CK10 33 /// /// CK11 86 55 5 CK12100 35 0 CK13 67 16 0 CK14 67 10 0 CK15 17 15 0 CK16 0 /// /// CK17 0/// /// CK20 57 /// /// CK21 80 25 10 CK22 0 /// /// CK23 0 /// /// CK250 /// /// CK26 0 /// /// CK27 0 /// /// CK28 0 /// /// CK29 0 /// ///CK30 0 /// /// CK32 0 /// /// CK33 29 /// /// CK34 0 /// /// CK35 0 ////// CK36 20 0 0 CK37 0 /// /// CK38 100 21 5 CK39 80 20 0 CK40 100 29 13CK41 86 53 0 CK42 0 /// /// CK43 0 /// /// CK44 80 25 10 CK45 86 12 0CK46 100 10 0 CK48 40 /// /// CK51 57 /// /// CK52 20 /// /// CK53 0 ////// CK55 0 /// /// CK56 0 /// /// CK57 0 /// /// CK58 0 /// /// CK59 57/// /// CK60 86 25 15 CK61 0 /// /// CK63 57 /// /// CK65 86 35 5 CK66 0/// /// CK67 14 /// /// CK68 14 /// /// CK69 100 5 0 CK70 0 /// /// CK710 /// /// CK72 0 /// /// CK74 0 /// /// CK75 0 /// /// CK76 0 /// ///CK77 0 /// /// CK78 0 /// /// CK79 0 /// /// CK80 0 /// /// CK81 0 ////// CK82 17 /// /// CK83 17 /// /// CK84 0 /// /// diflumetorim 0 //////

TABLE 307 contrastive tests against armyworm Insecticidal activityagainst armyworm (%) Compound No. 600 mg/L 100 mg/L 10 mg/L I-255 100100 25 I-3309 100 100 60 I-6756 100 100 28 I-6757 100 100 28 II-204 100100 47 II-297 100 95 30 II-482 100 100 80 II-8915 100 95 44 II-8965 100100 69 II-19334 100 84 44 III-22 100 100 71 III-187 100 100 95 III-199100 100 64 III-202 100 100 65 III-547 100 100 95 III-556 100 75 45III-562 100 100 83 CK4 40 /// /// CK5 100 56 0 CK6 29 /// /// CK7 100 00 CK8 17 /// /// CK9 40 /// /// CK10 0 /// /// CK11 29 /// /// CK12 8620 0 CK13 86 0 0 CK14 0 /// /// CK15 0 /// /// CK16 0 /// /// CK17 0 ////// CK18 100 43 14 CK19 86 25 7 CK20 /// /// 0 CK21 0 /// /// CK22 0 ////// CK23 0 /// /// CK24 /// /// 0 CK25 0 /// /// CK26 0 /// /// CK27 29/// /// CK28 29 /// /// CK29 14 /// /// CK30 57 /// /// CK32 0 /// ///CK33 100 0 0 CK34 0 /// /// CK35 0 /// /// CK36 0 /// /// CK37 0 /// ///CK38 0 /// /// CK39 0 /// /// CK40 43 6 0 CK41 100 0 0 CK42 0 /// ///CK43 0 /// /// CK44 0 /// /// CK45 0 /// /// CK46 71 0 0 CK47 86 25 0CK48 50 /// /// CK49 17 /// /// CK51 43 /// /// CK52 0 /// /// CK53 0/// /// CK54 67 /// /// CK55 0 /// /// CK56 0 /// /// CK57 0 /// ///CK58 0 /// /// CK59 14 /// /// CK60 0 /// /// CK61 0 /// /// CK63 71 ////// CK64 0 /// /// CK65 0 /// /// CK66 0 /// /// CK67 0 /// /// CK68 0/// /// CK70 0 /// /// CK71 86 /// /// CK72 71 /// /// CK73 100 50 0CK74 0 /// /// CK75 0 /// /// CK76 0 /// /// CK77 0 /// /// CK78 0 ////// CK79 0 /// /// CK80 0 /// /// CK81 14 /// /// CK82 0 /// /// CK83 29/// /// CK84 0 /// /// diflumetorim 0 /// ///

TABLE 308 contrastive tests against peach aphid Insecticidal activityagainst peach aphid (%) Compound 600 100 10 5 2.5 1.25 No. mg/L mg/Lmg/L mg/L mg/L mg/L I-22 100 100 100 100 100 100 I-254 100 100 100 100100 100 I-3309 100 100 100 100 96 48 I-6731 100 100 100 100 93 60 I-6735100 100 100 100 80 67 I-6739 100 100 100 100 100 100 I-6756 100 100 100100 100 100 I-6757 100 100 100 100 100 100 I-6758 100 100 100 100 100 89I-6765 100 100 100 100 100 84 II-19 100 100 100 /// /// /// II-69 100100 100 100 81 /// II-204 100 100 100 100 97 60 II-297 100 100 100 100100 93 II-347 100 100 100 100 100 81 II-482 100 100 100 100 100 100II-1687 100 100 100 /// /// /// II-1965 100 100 100 /// /// /// II-8915100 100 100 100 100 100 II-8917 100 100 100 83 /// /// II-8965 100 100100 91 /// /// II-10583 100 100 100 /// /// /// II-19334 100 100 100 9683 67 III-7 100 100 90 88 /// /// III-22 100 100 100 100 98 67 III-181100 100 100 /// /// /// III-187 100 100 100 /// /// /// III-202 100 100100 100 100 94 III-301 100 100 100 /// /// /// III-547 100 100 100 ////// /// III-562 100 100 100 /// /// /// CK2 100 100 95 37 23 0 CK4 100100 64 41 0 /// CK6 100 76 0 /// /// /// CK7 100 100 59 /// /// /// CK80 /// /// /// /// /// CK9 100 79 23 /// /// /// CK10 100 91 23 /// ////// CK11 100 98 85 25 0 /// CK12 100 100 73 /// /// /// CK13 100 98 83 0/// /// CK14 100 70 0 /// /// /// CK15 69 40 0 /// /// /// CK16 64 ////// /// /// /// CK17 0 /// /// /// /// /// CK18 100 71 51 7 0 /// CK19100 86 33 /// /// /// CK21 100 98 35 19 0 /// CK22 0 /// /// /// /// ///CK23 0 /// /// /// /// /// CK24 100 100 89 28 0 /// CK25 0 /// /// ////// /// CK26 100 48 45 /// /// /// CK27 0 /// /// /// /// /// CK28 100100 43 /// /// /// CK29 0 /// /// /// /// /// CK30 93 50 0 /// /// ///CK32 0 /// /// /// /// /// CK33 0 /// /// /// /// /// CK34 65 /// ////// /// /// CK35 0 /// /// /// /// /// CK36 90 14 0 /// /// /// CK37 10016 0 /// /// /// CK38 100 24 0 /// /// /// CK39 100 86 2 0 /// /// CK40100 100 72 27 0 /// CK41 100 97 23 15 0 /// CK42 100 67 20 17 0 /// CK430 /// /// /// /// /// CK44 100 98 35 19 0 /// CK45 100 98 55 39 26 0CK46 100 5 0 /// /// /// CK48 100 87 0 /// /// /// CK51 100 50 0 /// ////// CK52 88 0 0 /// /// /// CK53 84 66 34 /// /// /// CK54 100 100 34/// /// /// CK55 0 /// /// /// /// /// CK56 100 0 0 /// /// /// CK57 61/// /// /// /// /// CK58 100 0 0 /// /// /// CK59 75 15 0 /// /// ///CK60 81 0 0 /// /// /// CK61 88 0 0 /// /// /// CK63 100 0 0 /// /// ///CK65 0 /// /// /// /// /// CK66 0 /// /// /// /// /// CK67 86 54 0 ////// /// CK68 0 /// /// /// /// /// CK69 100 100 70 /// /// /// CK70 81 00 /// /// /// CK72 55 /// /// /// /// /// CK73 100 100 0 /// /// ///CK74 100 100 26 /// /// /// CK75 100 0 0 /// /// /// CK76 52 /// /// ////// /// CK77 72 /// /// /// /// /// CK78 0 /// /// /// /// /// CK79 10016 0 /// /// /// CK80 87 40 16 /// /// /// CK81 75 /// /// /// /// ///CK82 86 130 0 /// /// /// CK83 100 100 11 /// /// /// CK84 100 43 7 ////// /// diflumetorim 100 35 0 /// /// /// flufenerim 100 100 100 100 9037

TABLE 309 contrastive tests against carmine spider mite Insecticidalactivity against Compound carmine spider mite (% ) No. 600 mg/L 100 mg/L10 mg/L I-22 100 100 74 I-254 100 100 97 I-255 100 100 85 I-987 100 10080 I-6729 100 100 87 I-6734 100 100 82 I-6757 100 100 97 I-6758 100 10099 I-6739 100 100 100 I-6756 100 100 100 I-6741 100 100 85 I-6765 100100 100 I-6740 100 100 85 II-69 100 100 90 II-204 100 100 100 II-297 100100 74 II-299 100 100 72 II-347 100 100 100 II-432 100 100 76 II-443 100100 83 II-482 100 100 100 II-8965 100 100 100 II-19334 100 100 100 III-7100 100 /// III-16 100 100 /// III-22 100 100 72 III-181 100 100 ///III-199 100 100 87 III-547 100 100 /// III-556 100 100 /// III-559 100100 /// III-562 100 100 88 CK2 100 100 32 CK4 75 /// /// CK6 100 53 5CK7 100 96 36 CK8 54 /// /// CK12 100 41 /// CK13 100 0 0 CK14 100 33 6CK15 59 0 0 CK16 0 /// /// CK17 40 /// /// CK20 100 72 /// CK21 0 ////// CK23 64 /// /// CK24 100 100 85 CK25 0 /// /// CK26 0 /// /// CK27100 100 18 CK28 100 100 22 CK30 100 100 28 CK32 91 22 0 CK33 41 /// ///CK34 0 /// /// CK35 0 /// /// CK36 0 /// /// CK37 0 /// /// CK38 99 3714 CK39 100 37 16 CK41 100 99 0 CK43 74 29 16 CK44 0 /// /// CK45 0 ////// CK46 100 63 28 CK52 44 /// /// CK53 100 100 12 CK55 0 /// /// CK5632 25 0 CK57 33 /// /// CK58 0 /// /// CK59 0 /// /// CK60 0 /// ///CK61 0 /// /// CK62 0 /// /// CK63 0 /// /// CK64 56 /// /// CK65 0 ////// CK66 0 /// /// CK67 61 /// /// CK68 4 /// /// CK69 100 100 4 CK70 13/// /// CK72 13 /// /// CK73 100 85 24 CK74 0 /// /// CK75 0 /// ///CK76 41 /// /// CK77 56 /// /// CK78 17 /// /// CK79 27 /// /// CK80 6/// /// CK81 0 /// /// CK82 23 /// /// CK84 100 0 0 diflumetorim 100 10073 flufenerim 100 100 72

Further contrastive tests were carried out between the compounds withbetter activities, such as compound I-22, I-254, I-255, I-6729, I-6734,I-6739, I-6756, I-6757, I-6758, II-204, II-347, II-482, II-8965 andII-19334, and the contrast CK24 at a low dosage. The test results arelisted in table 310.

TABLE 310 Insecticidal activity against carmine spider mite (%) CompoundNo. 5 mg/L 2.5 mg/L I-22 59 /// I-254 93 79 I-255 84 72 I-6729 78 64I-6734 57 51 I-6739 93 76 I-6756 88 71 I-6757 80 75 I-6758 82 79 II-20480 60 II-347 90 75 II-482 100 93 II-8965 92 82 II-19334 100 87 CK24 15 5

We claim:
 1. A substituted pyrimidine compound represented by formulaPY:

wherein R₁ is cyano, C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₂-C₁₂alkenyl, haloC₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl, ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl; R₂ is halo, cyano,C₃-C₁₂cycloalkyl, C₁-C₁₂alkyl, or haloC₁-C₁₂alkoxy; R₃ and R₄, may bethe same or different, and are each selected independently from thegroup consisting of H, halo, OH, amino, C₁-C₁₂alkyl, C₁-C₁₂alkoxy,C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, unsubstituted or furthersubstituted arylC₁-C₆alkyl or heteroarylC₁-C₆alkyl by 1 to 5 followinggroups: halo, C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy, andhaloC₁-C₆alkoxy; or R₃, R₄ and conjoint carbon can also form a C₃-C₈cycle; R_(5a), R_(5b), and R_(5c), may be the same or different, and areeach selected independently from the group consisting of H, OH,C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio, haloC₁-C₁₂alkylthio, C₃-C₁₂alkenoxy,haloC₃-C₁₂alkenoxy, C₃-C₁₂alkynoxy, haloC₃-C₁₂alkynoxy,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl,C₁-C₁₂alkylcarbonyloxy, C₁-C₁₂alkylcarbonylamino,C₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkoxycarbonylamino,C₁-C₁₂alkoxyC₁-C₁₂alkoxy, and C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy; X₁ is Nor CR₆; X₂ is N or CR₇; X₃ is N or CR₈; X₄ is N or CR₉; X₅ is N or CR₁₀;X₆ is N or CR₁₁; however, X₂, X₃, X₄, X₅, X₆ are not simultaneously N;R₆ is selected from H, OH, HO(C═O), amino, C₃-C₁₂cycloalkyl,C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy,C₁-C₁₂alkylthio, haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, halodi(C₁-C₁₂alkyl)amino, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,di(C₁-C₁₂alkyl)amino(C₁-C₁₂alkyl), CONH₂, CONHNH₂, CON(C₁-C₁₂alkyl)NH₂,CONHNH(C₁-C₁₂alkyl), CONHN(di(C₁-C₁₂alkyl)), CONHNHCO(C₁-C₁₂alkyl),CONHNHCO₂(C₁-C₁₂alkyl), CONHNH(phenyl), C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, halodi(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkylsulfonyl(C₁-C₁₂alkyl)amino,haloC₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkoxyamino,C₁-C₁₂alkoxycarbonylamino, C₁-C₁₂alkoxyaminocarbonyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl,di(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylcarbonyloxy,haloC₁-C₁₂alkylcarbonyloxy, C₁-C₁₂alkoxycarbonyloxy,haloC₁-C₁₂alkoxycarbonyloxy, C₁-C₁₂alkylaminocarbonyloxy,haloC₁-C₁₂alkylaminocarbonyloxy, C₁-C₁₂alkylsulfonyloxy,haloC₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxyC₁-C₁₂alkoxy,haloC₁-C₁₂alkoxyC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy orhaloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy; R₇, R₈, R₉, R₁₀, and R₁₁, may bethe same or different, and are each selected independently from thegroup consisting of H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₁₂alkyl, haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy,C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy,haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, halodi(C₁-C₁₂alkyl)amino, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,di(C₁-C₁₂alkyl)amino(C₁-C₁₂alkyl), CONH₂, CONHNH₂, CON(C₁-C₁₂alkyl)NH₂,CONHNH(C₁-C₁₂alkyl), CONHN(di(C₁-C₁₂alkyl)), CONHNHCO(C₁-C₁₂alkyl),CONHNHCO₂(C₁-C₁₂alkyl), CONHNH(phenyl), C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, halodi(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkylsulfonyl(C₁-C₁₂alkyl)amino,haloC₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkoxyamino,C₁-C₁₂alkoxycarbonylamino, C₁-C₁₂alkoxyaminocarbonyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl,di(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylcarbonyloxy,haloC₁-C₁₂alkylcarbonyloxy, C₁-C₁₂alkoxycarbonyloxy,haloC₁-C₁₂alkoxycarbonyloxy, C₁-C₁₂alkylaminocarbonyloxy,haloC₁-C₁₂alkylaminocarbonyloxy, C₁-C₁₂alkyl sulfonyloxy,haloC₁-C₁₂alkyl sulfonyloxy, C₁-C₁₂alkoxyC₁-C₁₂alkoxy,haloC₁-C₁₂alkoxyC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy, andhaloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy; W is H, halo, C₁-C₁₂alkyl,C₁-C₁₂alkylthio, or C₁-C₁₂alkylsulfonyl; A is NR₁₂; B is —CH₂— or—CH₂CH₂—; and R₁₂ is H, OH, H(C)═O, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylaminosulfonyl,di(C₁-C₁₂alkyl)aminosulfonyl, C₁-C₁₂alkylsulfonylaminocarbonyl,C₁-C₁₂alkylcarbonylaminosulfonyl, C₃-C₁₂cycloalkyloxycarbonyl,C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl,haloC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, C₂-C₁₂alkenoxycarbonyl,C₂-C₁₂alkynoxycarbonyl, C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylaminothio, di(C₁-C₁₂alkyl)aminothio, unsubstituted or furthersubstituted (hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, or (hetero)arylC₁-C₆alkyloxycarbonyl by 1 to 5following groups: halo, NO₂, cyano, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy, or haloC₁-C₆alkoxy; or a salt thereof formed with an acidselected from the group consisting of hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, formic acid, acetic acid, trifluoroaceticacid, oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoicacid, alizaric acid, maleic acid, sorbic acid, malic acid, and citricacid.
 2. The substituted pyrimidine compound according to claim 1,wherein the substituted pyrimidine compound is represented by formula I:

wherein R₁ is cyano, C₃-C₁₂cycloalkyl, C₁-C₁₂alkyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl, ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl; R₂ is halo, cyano,C₃-C₁₂cycloalkyl, or C₁-C₁₂alkyl; R₃ and R₄, may be the same ordifferent, and are each selected independently from the group consistingof H, halo, OH, amino, C₁-C₁₂alkyl, and C₁-C₁₂alkoxy; R_(5a), R_(5b),and R_(5c), may be the same or different, and are each selectedindependently from the group consisting of H or OH; X₂ is N or CR₇, X₃is N or CR₈, X₆ is N or CR₁₁, within X₂, X₃, X₆, at least onesubstituent is N; R₉ is H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₁₂alkyl, haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy,C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy,haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, C₁-C₁₂alkoxycarbonyl,di(C₁-C₁₂alkyl)amino(C₁-C₁₂alkyl), haloC₁-C₁₂alkoxycarbonyl, CONH₂,CONHNH₂, CON(C₁-C₁₂alkyl)NH₂, CONHNH(C₁-C₁₂alkyl),CONHN(di(C₁-C₁₂alkyl)), CONHNHCO(C₁-C₁₂alkyl), CONHNHCO₂(C₁-C₁₂alkyl),CONHNH(phenyl), C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkylsulfonyl(C₁-C₁₂alkyl)amino,haloC₁-C₁₂alkylsulfonylamino, C₁-C₁₂alkoxyamino,C₁-C₁₂alkoxycarbonylamino, C₁-C₁₂alkoxyaminocarbonyl, cyanoC₁-C₁₂alkyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl, ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl; R₆ is selected from H, OH,HO(C═O), amino, C₃-C₁₂cycloalkyl, C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy,C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino, di(C₁-C₁₂alkyl)amino,C₁-C₁₂alkoxycarbonyl, CONH₂, C₁-C₁₂alkylaminocarbonyl ordi(C₁-C₁₂alkyl)aminocarbonyl; R₇, R₈, R₁₀, and R₁₁, may be the same ordifferent, and are each selected independently from the group consistingof H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl,C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy,C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino, di(C₁-C₁₂alkyl)amino,C₁-C₁₂alkoxycarbonyl, CONH₂, C₁-C₁₂alkylaminocarbonyl, anddi(C₁-C₁₂alkyl)aminocarbonyl; W is H or C₁-C₁₂alkyl; A is NR₁₂; B is—CH₂— or —CH₂CH₂—; and R₁₂ is H, OH, H(C)═O, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl,C₁-C₁₂alkylthio, C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkenyl, haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, di(C₁-C₁₂alkyl)aminosulfonyl,C₁-C₁₂alkylsulfonylaminocarbonyl, C₁-C₁₂alkylcarbonylaminosulfonyl,C₃-C₁₂cycloalkyloxycarbonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,C₂-C₁₂alkenoxycarbonyl, C₂-C₁₂alkynoxycarbonyl,C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylaminothio,di(C₁-C₁₂alkyl)aminothio, unsubstituted or further substituted(hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, or (hetero)arylC₁-C₆alkyloxycarbonyl by 1 to 5following groups: halo, NO₂, cyano, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy, or haloC₁-C₆alkoxy; or a salt thereof formed with an acidselected from the group consisting of hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, formic acid, acetic acid, trifluoroaceticacid, oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoicacid, alizaric acid, maleic acid, sorbic acid, malic acid, and citricacid.
 3. The substituted pyrimidine compound according to claim 2,wherein R₁ is cyano, C₃-C₆cycloalkyl, C₁-C₆alkyl, cyanoC₁-C₆alkyl,cyanoC₁-C₆alkoxy, C₁-C₆alkoxycarbonylC₁-C₆alkyl,C₁-C₆alkylaminocarbonylC₁-C₆alkyl, ordi(C₁-C₆alkyl)aminocarbonylC₁-C₆alkyl; R₂ is halo, cyano,C₃-C₆cycloalkyl, or C₁-C₆alkyl; R₃ and R₄, may be the same or different,and are each selected independently from the group consisting of H,halo, OH, amino, C₁-C₆alkyl, and C₁-C₆alkoxy; R_(5a), R_(5b), andR_(5c), may be the same or different, selected independently from H orOH; X₂ is N or CR₇, X₃ is N or CR₈, X₆ is N or CR₁₁, within X₂, X₃, X₆,at least one substituent is N; R₆ is H; R₇ is H, halo, cyano, orC₁-C₆alkyl; R₈ is selected from the group consisting of H, halo, cyano,C₁-C₆alkyl, and C₁-C₆alkoxy; R₉ is H, halo, OH, cyano, HO(C═O), amino,NO₂, C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy, haloC₁-C₆alkoxy,C₃-C₆cycloalkyl, C₂-C₆alkenyl, C₂-C₆alkynyl, C₂-C₆alkenoxy,haloC₂-C₆alkenoxy, C₂-C₆alkynoxy, haloC₂-C₆alkynoxy, C₁-C₆alkylthio,haloC₁-C₆alkylthio, C₁-C₆alkoxyC₁-C₆alkyl, haloC₁-C₆alkoxyC₁-C₆alkyl,C₁-C₆alkylthioC₁-C₆alkyl, haloC₁-C₆alkylthioC₁-C₆alkyl,C₁-C₆alkylsulfinyl, haloC₁-C₆alkylsulfinyl, C₁-C₆alkylsulfonyl,haloC₁-C₆alkylsulfonyl, C₁-C₆alkylaminosulfonyl, C₁-C₆alkylamino,haloC₁-C₆alkylamino, di(C₁-C₆alkyl)amino, C₁-C₆alkoxycarbonyl, CONH₂,C₁-C₆alkylaminocarbonyl, di(C₁-C₆alkyl)aminocarbonyl, cyanoC₁-C₆alkoxy,C₁-C₆alkoxycarbonylC₁-C₆alkyl, C₁-C₆alkylaminocarbonylC₁-C₆alkyl, ordi(C₁-C₆alkyl)aminocarbonylC₁-C₆alkyl; R₁₀ is H, halo, OH, cyano,HO(C═O), amino, NO₂, C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy,haloC₁-C₆alkoxy, C₃-C₆cycloalkyl, C₂-C₆alkenyl, C₂-C₆alkynyl,C₂-C₆alkenoxy, haloC₂-C₆alkenoxy, C₂-C₆alkynoxy, haloC₂-C₆alkynoxy,C₁-C₆alkylthio, haloC₁-C₆alkylthio, C₁-C₆alkoxyC₁-C₆alkyl,haloC₁-C₆alkoxyC₁-C₆alkyl, C₁-C₆alkylthioC₁-C₆alkyl,haloC₁-C₆alkylthioC₁-C₆alkyl, C₁-C₆alkylsulfinyl,haloC₁-C₆alkylsulfinyl, C₁-C₆alkylsulfonyl, haloC₁-C₆alkylsulfonyl,C₁-C₆alkylamino, haloC₁-C₆alkylamino, di(C₁-C₆alkyl)amino,C₁-C₆alkoxycarbonyl, CONH₂, C₁-C₆alkylaminocarbonyl, ordi(C₁-C₆alkyl)aminocarbonyl; R₁₁ is H, halo, OH, cyano, HO(C═O), amino,NO₂, C₁-C₆alkyl, haloC₁-C₆alkyl, C₁-C₆alkoxy, haloC₁-C₆alkoxy,C₁-C₆alkoxycarbonyl, CONH₂, C₁-C₆alkylaminocarbonyl, ordi(C₁-C₆alkyl)aminocarbonyl; W is H or C₁-C₆alkyl; A is NR₁₂; B is —CH₂—or —CH₂CH₂—; and R₁₂ is H, OH, H(C)═O, C₁-C₆alkyl, C₁-C₆alkylcarbonyl,or C₁-C₆alkylsulfonyl; or wherein the salt of formula I is formed withhydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, formicacid, acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonicacid, p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid,sorbic acid, malic acid, or citric acid.
 4. The substituted pyrimidinecompound according to claim 3, wherein the substituted pyrimidinecompound is represented by formula I-A, I-B, I-C, I-D, I-E, I-F, I-G, orI-H:

wherein R₁ is cyano or C₁-C₄alkyl; R₂ is halo, cyano, C₃-C₄cycloalkyl,or C₁-C₄alkyl; R₃ and R₄, may be the same or different, and are eachselected independently from the group consisting of H, halo, OH, amino,C₁-C₄alkyl, and C₁-C₄alkoxy; R_(5b) is H or OH; R₇ is H, halo, cyano, orC₁-C₄alkyl; R₈ is H, halo, cyano, C₁-C₄alkyl, or C₁-C₄alkoxy; R₉ is H,halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl,C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkylthio, haloC₁-C₄alkylthio,C₁-C₄alkoxyC₁-C₄alkyl, haloC₁-C₄alkoxyC₁-C₄alkyl,C₁-C₄alkylthioC₁-C₄alkyl, haloC₁-C₄alkylthioC₁-C₄alkyl,C₁-C₄alkylsulfinyl, haloC₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl,haloC₁-C₄alkylsulfonyl, C₁-C₄alkylaminosulfonyl, C₁-C₄alkylamino,haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino, C₁-C₄alkoxycarbonyl, CONH₂,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl, cyanoC₁-C₄alkoxy,C₁-C₄alkoxycarbonylC₁-C₄alkyl, C₁-C₄alkylaminocarbonylC₁-C₄alkyl, ordi(C₁-C₄alkyl)aminocarbonylC₁-C₄alkyl; R₁₀ is H, halo, OH, cyano,HO(C═O), amino, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy,haloC₁-C₄alkoxy, C₃-C₄cycloalkyl, C₂-C₄alkenyl, C₂-C₄alkynyl,C₂-C₄alkenoxy, haloC₂-C₄alkenoxy, C₂-C₄alkynoxy, haloC₂-C₄alkynoxy,C₁-C₄alkylthio, haloC₁-C₄alkylthio, C₁-C₄alkoxyC₁-C₄alkyl,haloC₁-C₄alkoxyC₁-C₄alkyl, C₁-C₄alkylthioC₁-C₄alkyl,haloC₁-C₄alkylthioC₁-C₄alkyl, C₁-C₄alkylsulfinyl,haloC₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl, haloC₁-C₄alkylsulfonyl,C₁-C₄alkylamino, haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino,C₁-C₄alkoxycarbonyl, CONH₂, C₁-C₄alkylaminocarbonyl, ordi(C₁-C₄alkyl)aminocarbonyl; and R₁₁ is H, halo, OH, cyano, HO(C═O),amino, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₁-C₄alkoxycarbonyl, CONH₂, C₁-C₄alkylaminocarbonyl, ordi(C₁-C₄alkyl)aminocarbonyl; or the salt of formula I-A, I-B, I-C, I-D,I-E, I-F, I-G, or I-H is formed with hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, acetic acid, trifluoroacetic acid, oxalicacid, methylsulfonic acid, p-toluenesulfonic acid, benzoic acid, maleicacid, sorbic acid, malic acid, or citric acid.
 5. The substitutedpyrimidine compound according to claim 4, wherein R₁ is cyano, CH₃,C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉, or t-C₄H₉; R₂ is F, Cl,Br, cyano, CH₃, or C₂H₅; R₃ and R₄, may be the same or different, andare each selected independently from the group consisting of H, Cl, Br,OH, amino, CH₃, C₂H₅, OCH₃, and OC₂H₅; R_(5b) is H or OH; R₇ is H, Cl,or cyano; R₈ is H, Cl, Br, cyano, CH₃, or OCH₃; R₉ is H, F, Cl, Br,cyano, HO(C═O), amino, NO₂, CH₃, C₂H₅, CF₃, CClF₂, OCH₃, OC₂H₅, OCF₃,COOCH₃, COOC₂H₅, CONH₂, CONHCH₃, CONHC₂H₅, CON(CH₃)₂, SO₂CH₃, orSO₂NHCH₃; R₁₀ is H, Cl, cyano, CH₃, C₂H₅, OCH₃, or OC₂H₅; and R₁₁ is H,F, Cl, Br, cyano, HO(C═O), amino, NO₂, CH₃, C₂H₅, CF₃, CClF₂, OCH₃,OC₂H₅, OCF₃, COOCH₃, COOC₂H₅, CONH₂, CONHCH₃, CONHC₂H₅, or CON(CH₃)₂; orthe salt of formula I-A, I-B, I-C, I-D, I-E, I-F, I-G, or I—H is formedwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, maleic acid, or benzoic acid.
 6. The substitutedpyrimidine compound according to claim 5, wherein the substitutedpyrimidine compound is represented by formula I-A and wherein R₁ is CH₃or C₂H₅; R₂ is Cl, Br, or cyano; R₃, R₄, and R₁₀ are H; R_(5b) is H; R₈is H or Cl; R₉ is H, Cl, cyano, CF₃, CClF₂, COOCH₃, COOC₂H₅, or CONH₂;and R₁₁ is H, Cl, NO₂, CF₃, COOCH₃, or CONHCH₃; or wherein thesubstituted pyrimidine compound is represented by formula I-B and R₁ isCH₃, C₂H₅, or CHF₂; R₂ is Cl, Br, or cyano; R₉ is Cl, Br, cyano, or CF₃;and R₃, R₄, R_(5b), R₁₀, and R₁₁ are H; or wherein the substitutedpyrimidine compound is represented by formula I-C and R₁ is CH₃, C₂H₅,or CHF₂; R₂ is Cl, Br, or cyano; R₃, R₄, R_(5b), and R₉ are H; and R₈and R₁₀ are CH₃ or OCH₃; or wherein the substituted pyrimidine compoundis represented by formula I-D and R₁ is CH₃, C₂H₅, or CHF₂; R₂ is Cl,Br, or cyano; R₃, R₄, R_(5b), R₈, and R₁₀ are H; R₉ is H, Cl, cyano,CF₃, COOCH₃, COOC₂H₅, or CONH₂; and R₁₁ is H, Cl, or CF₃; or wherein thesalt of formula I-A, I-B, I-C, or I-D is formed with hydrochloric acid,sulfuric acid, nitric acid, phosphoric acid, acetic acid,trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, maleic acid, or benzoic acid.
 7. The substitutedpyrimidine compound according to claim 6, wherein the substitutedpyrimidine compound is represented by formula I-A and wherein R₁ is CH₃or C₂H₅; R₂ is Cl, Br, or cyano; R₃, R₄, R_(5b), and R₁₀ are H; R₉ isCl, cyano, or CF₃; and R₈ and R₁₁ are H or Cl; or wherein thesubstituted pyrimidine compound is represented by formula I-B and R₁ isCH₃, C₂H₅, or CHF₂; R₂ and R₉ are Cl, Br, or cyano; and R₃, R₄, R_(5b),R₁₀, and R₁₁ are H; or wherein the salt of formula I-A or I-B is formedwith hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonic acid,p-toluenesulfonic acid, maleic acid, or benzoic acid.
 8. A substitutedpyrimidine compound represented by formula II:

wherein R₁ is C₁-C₁₂alkyl or C₃-C₈cycloalkyl; R₂ is halo or cyano; R₃and R₄, may be the same or different, and are each selectedindependently from the group consisting of H, halo, C₁-C₁₂alkyl,C₁-C₁₂alkoxy, and C₃-C₁₂cycloalkyl; or R₃, R₄ and conjoint carbon canalso form a C₃-C₈ cycle; R_(5a), R_(5b), and R_(5c), may be the same ordifferent, and are each selected independently from the group consistingof H or OH; R₆ is selected from H, OH, amino, C₃-C₁₂ cycloalkyl,C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino, di(C₁-C₁₂alkyl)amino,halodi(C₁-C₁₂alkyl)amino, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, halodi(C₁-C₁₂alkyl)aminocarbonyl, CONH₂,C₁-C₁₂alkylthio, haloC₁-C₁₂alkylthio, C₂-C₁₂alkenoxy,haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy,C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, haloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylcarbonyloxy,haloC₁-C₁₂alkylcarbonyloxy C₁-C₁₂alkoxycarbonyloxy,haloC₁-C₁₂alkoxycarbonyloxy, C₁-C₁₂alkylaminocarbonyloxy,haloC₁-C₁₂alkylaminocarbonyloxy, C₁-C₁₂alkylsulfonyloxy,haloC₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxyC₁-C₁₂alkoxy,haloC₁-C₁₂alkoxyC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy orhaloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy; R₇, R₈, R₉, R₁₀, and R₁₁, may bethe same or different, and are each selected independently from thegroup consisting of H, halo, OH, amino, cyano, NO₂, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂ cycloalkyl,C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino, di(C₁-C₁₂alkyl)amino,halodi(C₁-C₁₂alkyl)amino, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, halodi(C₁-C₁₂alkyl)aminocarbonyl, CONH₂,C₁-C₁₂alkylthio, haloC₁-C₁₂alkylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy,C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, haloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl,haloC₁-C₁₂alkylthiocarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylcarbonyloxy,haloC₁-C₁₂alkylcarbonyloxy, C₁-C₁₂alkoxycarbonyloxy,haloC₁-C₁₂alkoxycarbonyloxy, C₁-C₁₂alkylaminocarbonyloxy,haloC₁-C₁₂alkylaminocarbonyloxy, C₁-C₁₂alkyl sulfonyloxy,haloC₁-C₁₂alkyl sulfonyloxy, C₁-C₁₂alkoxyC₁-C₁₂alkoxy,haloC₁-C₁₂alkoxyC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy, andhaloC₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy; W is H or C₁-C₁₂alkyl; A is NR₁₂;B is —CH₂— or —CH₂CH₂—; and R₁₂ is H, OH, H(C)═O, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl,C₁-C₁₂alkylthio, C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkenyl, haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, di(C₁-C₁₂alkyl)aminosulfonyl,C₁-C₁₂alkylsulfonylaminocarbonyl, C₁-C₁₂alkylcarbonylaminosulfonyl,C₃-C₁₂cycloalkyloxycarbonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl, haloC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,C₂-C₁₂alkenoxycarbonyl, C₂-C₁₂alkynoxycarbonyl,C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylaminothio,di(C₁-C₁₂alkyl)aminothio, unsubstituted or further substituted(hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, or (hetero)arylC₁-C₆alkyloxycarbonyl by 1 to 5following groups: halo, NO₂, cyano, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy, or haloC₁-C₆alkoxy; or a salt thereof formed with an acidselected from the group consisting of hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, formic acid, acetic acid, trifluoroaceticacid, oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoicacid, alizaric acid, maleic acid, sorbic acid, malic acid, and citricacid.
 9. The substituted pyrimidine compound according to claim 8,wherein R₁ is C₁-C₆alkyl or C₃-C₆cycloalkyl; R₂ is halo or cyano; R₃ andR₄, may be the same or different, and are each selected independentlyfrom the group consisting of H, halo, C₁-C₆alkyl, C₁-C₆alkoxy, andC₃-C₆cycloalkyl; or R₃, R₄ and conjoint carbon can also form a C₃-C₈cycle; R_(5a), R_(5b), and R_(5c), may be the same or different,selected independently from H or OH; R₆ is H or OH; R₇, R₈, R₉, R₁₀, andR₁₁, may be the same or different, and are each selected independentlyfrom the group consisting of H, halo, OH, amino, cyano, NO₂, C₁-C₆alkyl,haloC₁-C₆alkyl, C₁-C₆alkoxy, haloC₁-C₆alkoxy, C₃-C₆cycloalkyl,C₁-C₆alkylamino, haloC₁-C₆alkylamino, di(C₁-C₆alkyl)amino,halodi(C₁-C₆alkyl)amino, C₁-C₆alkylaminocarbonyl,di(C₁-C₆alkyl)aminocarbonyl, halodi(C₁-C₆alkyl)aminocarbonyl, CONH₂,C₁-C₆alkylthio, haloC₁-C₆alkylthio, C₂-C₆alkenyl, C₂-C₆alkynyl,C₂-C₆alkenoxy, haloC₂-C₆alkenoxy, C₂-C₆alkynoxy, haloC₂-C₆alkynoxy,C₁-C₆alkylsulfonyl, haloC₁-C₆alkylsulfonyl, C₁-C₆alkylcarbonyl,haloC₁-C₆alkylcarbonyl, C₁-C₆alkoxycarbonyl, haloC₁-C₆alkoxycarbonyl,C₁-C₆alkoxyC₁-C₆alkyl, haloC₁-C₆alkoxyC₁-C₆alkyl,C₁-C₆alkylthioC₁-C₆alkyl, haloC₁-C₆alkylthioC₁-C₆alkyl,C₁-C₆alkoxycarbonylC₁-C₆alkyl, haloC₁-C₆alkoxycarbonylC₁-C₆alkyl,C₁-C₆alkylthiocarbonylC₁-C₆alkyl, haloC₁-C₆alkylthiocarbonylC₁-C₆alkyl,C₁-C₆alkylcarbonyloxy, haloC₁-C₆alkylcarbonyloxy,C₁-C₆alkoxycarbonyloxy, haloC₁-C₆alkoxycarbonyloxy,C₁-C₆alkylaminocarbonyloxy, haloC₁-C₆alkylaminocarbonyloxy,C₁-C₆alkylsulfonyloxy, haloC₁-C₆alkylsulfonyloxy,C₁-C₆alkoxyC₁-C₆alkoxy, haloC₁-C₆alkoxyC₁-C₆alkoxy,C₁-C₆alkoxycarbonylC₁-C₆alkoxy, and haloC₁-C₆alkoxycarbonylC₁-C₆alkoxy;W is H or C₁-C₃alkyl; A is NR₁₂; B is —CH₂— or —CH₂CH₂—; and R₁₂ is H,OH, H(C)═O, C₁-C₆alkyl, C₁-C₆alkylsulfonyl or C₁-C₆alkylcarbonyl; orwherein the salt is formed with hydrochloric acid, sulfuric acid, nitricacid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid,oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoic acid,alizaric acid, maleic acid, sorbic acid, malic acid, or citric acid. 10.The substituted pyrimidine compound according to claim 9, wherein R₁ isC₁-C₄alkyl or C₃-C₄cycloalkyl; R₂ is F, Cl, Br, or cyano; R₃ and R₄, maybe the same or different, and are each selected independently from thegroup consisting of H, halo, C₁-C₄alkyl, C₁-C₄alkoxy, andC₃-C₆cycloalkyl; or R₃, R₄ and conjoint carbon can also form a C₃-C₈cycle; R_(5a), R_(5b), and R_(5c), may be the same or different,selected independently from H or OH; R₆ is H or OH; R₇, R₈, R₉, R₁₀, andR₁₁, may be the same or different, and are each selected independentlyfrom the group consisting of H, halo, OH, amino, cyano, NO₂, C₁-C₄alkyl,haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₃-C₄cycloalkyl,C₁-C₄alkylamino, haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino,halodi(C₁-C₄alkyl)amino, C₁-C₄alkylaminocarbonyl,di(C₁-C₄alkyl)aminocarbonyl, halodi(C₁-C₄alkyl)aminocarbonyl, CONH₂,C₁-C₄alkylthio, haloC₁-C₄alkylthio, C₂-C₄alkenyl, C₂-C₄alkynyl,C₂-C₄alkenoxy, haloC₂-C₄alkenoxy, C₂-C₄alkynoxy, haloC₂-C₄alkynoxy,C₁-C₄alkylsulfonyl, haloC₁-C₄alkylsulfonyl, C₁-C₄alkylcarbonyl,haloC₁-C₄alkylcarbonyl, C₁-C₄alkoxycarbonyl, haloC₁-C₄alkoxycarbonyl,C₁-C₄alkoxyC₁-C₄alkyl, haloC₁-C₄alkoxyC₁-C₄alkyl,C₁-C₄alkylthioC₁-C₄alkyl, haloC₁-C₄alkylthioC₁-C₄alkyl,C₁-C₄alkoxycarbonylC₁-C₄alkyl, haloC₁-C₄alkoxycarbonylC₁-C₄alkyl,C₁-C₄alkylthiocarbonylC₁-C₄alkyl, haloC₁-C₄alkylthiocarbonylC₁-C₄alkyl,C₁-C₄alkylcarbonyloxy, haloC₁-C₄alkylcarbonyloxy,C₁-C₄alkoxycarbonyloxy, haloC₁-C₄alkoxycarbonyloxy,C₁-C₄alkylaminocarbonyloxy, haloC₁-C₄alkylaminocarbonyloxy,C₁-C₄alkylsulfonyloxy, haloC₁-C₄alkylsulfonyloxy,C₁-C₄alkoxyC₁-C₄alkoxy, haloC₁-C₄alkoxyC₁-C₄alkoxy,C₁-C₄alkoxycarbonylC₁-C₄alkoxy, and haloC₁-C₄alkoxycarbonylC₁-C₄alkoxy;W is H or CH₃; A is NR₁₂; B is —CH₂— or —CH₂CH₂—; and R₁₂ is H, OH,H(C)═O, C₁-C₄alkyl, C₁-C₄alkylsulfonyl, or C₁-C₄alkylcarbonyl; orwherein the salt is formed with hydrochloric acid, sulfuric acid, nitricacid, phosphoric acid, acetic acid, trifluoroacetic acid, oxalic acid,methylsulfonic acid, p-toluenesulfonic acid, benzoic acid, maleic acid,sorbic acid, malic acid, or citric acid.
 11. The substituted pyrimidinecompound according to claim 10, wherein R₁ is CH₃, C₂H₅, n-C₃H₇, i-C₃H₇,n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, cyclopropyl or cyclobutyl; R₂ is F, Cl,Br, or cyano; R₃ and R₄, may be the same or different, and are eachselected independently from the group consisting of H, F, Cl, Br, I,CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, OCH₃, OC₂H₅,OC₃H₇-n, OC₃H₇-i, OC₄H₉-n, OC₄H₉-s, OC₄H₉-i, and OC₄H₉-t; R_(5a),R_(5b), and R_(5c), may be the same or different, selected independentlyfrom H or OH; R₆ is H or OH; R₇, R₈, R₉, R₁₀, and R₁₁, may be the sameor different, and are each selected independently from the groupconsisting of H, F, Cl, Br, I, cyano, amino, NO₂, CH₃, C₂H₅, n-C₃H₇,i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, CF₃, CCl₃, CClF₂, CCl₂F, CHCl₂,CH₂F, CHF₂, OCH₃, OC₂H₅, OC₃H₇-n, OC₃H₇-i, OC₄H₉-n, OC₄H₉-s, OC₄H₉-i,OC₄H₉-t, OCF₃, OCH₂CF₃, COOCH₃, COOC₂H₅, CONH₂, CONHCH₃, CONHC₂H₅,CONH(CH₃)₂, methylsulfonyl, and trifluoromethylsulfonyl; W is H or CH₃;A is NR₁₂; B is —CH₂— or —CH₂CH₂—; and R₁₂ is H; or wherein the salt isformed with hydrochloric acid, sulfuric acid, nitric acid, phosphoricacid, acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonicacid, p-toluenesulfonic acid, maleic acid, or benzoic acid.
 12. Thesubstituted pyrimidine compound according to claim 11, wherein R₁ isCH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, cyclopropylor cyclobutyl; R₂ is F, Cl, Br, or cyano; R₃ and R₄, may be the same ordifferent, and are each selected independently from the group consistingof H, F, Cl, Br, I, CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, OCH₃, OC₂H₅, OC₃H₇-n, andOC₃H₇-i; R_(5a), R_(5b), and R_(5c), are H; R₆ is H; R₇, R₈, R₉, R₁₀,and R₁₁, may be the same or different, and are each selectedindependently from the group consisting of H, F, Cl, Br, I, cyano, NO₂,CH₃, C₂H₅, n-C₃H₇, i-C₃H₇, n-C₄H₉, s-C₄H₉, i-C₄H₉, t-C₄H₉, OCH₃, OCF₃,CF₃, CCl₃, CClF₂, CCl₂F, CHCl₂, CH₂F, CHF₂, methylsulfonyl, andtrifluoromethylsulfonyl; W is H or CH₃; A is NH; B is —CH₂— or —CH₂CH₂—;and or wherein the salt is formed with hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, acetic acid, trifluoroacetic acid, oxalicacid, methylsulfonic acid, p-toluenesulfonic acid, maleic acid, orbenzoic acid.
 13. The substituted pyrimidine compound according to claim12, wherein R₁ is CH₃ or C₂H₅; R₂ is Cl or cyano; R₃ and R₄ are H;R_(5a), R_(5b), and R_(5c), are H; R₆ is H; W is H or CH₃; R₇, R₈, R₉,R₁₀, and R₁₁, may be the same or different, and are each selectedindependently from the group consisting of H, F, Cl, cyano, NO₂, CH₃,OCH₃, OCF₃, CF₃, and methylsulfonyl; A is NH; and B is —CH₂— or—CH₂CH₂—; or wherein the salt is formed with hydrochloric acid, sulfuricacid, nitric acid, phosphoric acid, acetic acid, or trifluoroaceticacid.
 14. A substituted pyrimidine compound represented by formula III:

wherein R₁ is C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl,haloC₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkynyl,C₁-C₁₂alkoxyC₁-C₁₂alkyl, or haloC₁-C₁₂alkoxyC₁-C₁₂alkyl; R₂ is halo,cyano, C₁-C₁₂alkyl, or haloC₁-C₁₂alkoxy; W is H, halo, C₁-C₁₂alkyl,C₁-C₁₂alkylthio, or C₁-C₁₂alkylsulfonyl; R₃ and R₄, may be the same ordifferent, and are each selected independently from the group consistingof H, C₁-C₁₂alkyl, C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,haloC₂-C₁₂alkenyl, haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl,unsubstituted or further substituted arylC₁-C₆alkyl orheteroarylC₁-C₆alkyl by 1 to 5 following groups: halo, C₁-C₆alkyl,haloC₁-C₆alkyl, C₁-C₆alkoxy, and haloC₁-C₆alkoxy; or R₃, R₄ and conjointcarbon can also form a C₃-C₅₈ cycle; R_(5a), R_(5b), and R_(5c), may bethe same or different, and are each selected independently from thegroup consisting of H, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,haloC₁-C₁₂alkylthio, C₃-C₁₂alkenoxy, haloC₃-C₁₂alkenoxy, C₃-C₁₂alkynoxy,haloC₃-C₁₂alkynoxy, C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl,C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylcarbonyl,haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkylcarbonyloxy,C₁-C₁₂alkylcarbonylamino, C₁-C₁₂alkylsulfonyloxy, C₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkoxycarbonylamino,C₁-C₁₂alkoxyC₁-C₁₂alkoxy, and C₁-C₁₂alkoxycarbonylC₁-C₁₂alkoxy; X₂ is Nor CR₇; X₃ is N or CR₈; X₄ is N or CR₉; X₆ is N or CR₁₁; however, X₂,X₃, X₄, and X₆ are not simultaneously N; R₇, R₈, R₉, and R₁₁, may be thesame or different, and are each selected independently from the groupconsisting of H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₁₂alkyl,haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonyl,CONH₂, C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,C₁-C₁₂alkylsulfonyl, and haloC₁-C₁₂alkylsulfonyl; R₁₀ is H, halo, OH,cyano, HO(C═O), amino, NO₂, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl, C₁-C₁₂alkoxy,haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl,C₂-C₁₂alkenoxy, haloC₂-C₁₂alkenoxy, C₂-C₁₂alkynoxy, haloC₂-C₁₂alkynoxy,C₁-C₁₂alkylthio, haloC₁-C₁₂alkylthio, C₁-C₁₂alkoxyC₁-C₁₂alkyl,haloC₁-C₁₂alkoxyC₁-C₁₂alkyl, C₁-C₁₂alkylthioC₁-C₁₂alkyl,haloC₁-C₁₂alkylthioC₁-C₁₂alkyl, C₁-C₁₂alkylsulfinyl,haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl, haloC₁-C₁₂alkylsulfonyl,C₁-C₁₂alkylaminosulfonyl, C₁-C₁₂alkylamino, haloC₁-C₁₂alkylamino,di(C₁-C₁₂alkyl)amino, C₁-C₁₂alkoxycarbonyl, CONH₂,C₁-C₁₂alkylaminocarbonyl, di(C₁-C₁₂alkyl)aminocarbonyl,cyanoC₁-C₁₂alkoxy, C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl,C₁-C₁₂alkylaminocarbonylC₁-C₁₂alkyl, ordi(C₁-C₁₂alkyl)aminocarbonylC₁-C₁₂alkyl; A is NR₁₂; B is —CH₂— or—CH₂CH₂—; and R₁₂ is H, OH, H(C)═O, C₁-C₁₂alkyl, haloC₁-C₁₂alkyl,C₁-C₁₂alkoxy, haloC₁-C₁₂alkoxy, C₃-C₁₂cycloalkyl, C₁-C₁₂alkylthio,C₂-C₁₂alkenylthio, C₂-C₁₂alkenyl, C₂-C₁₂alkynyl, haloC₂-C₁₂alkenyl,haloC₂-C₁₂alkynyl, C₁-C₁₂alkoxyC₁-C₁₂alkyl, haloC₁-C₁₂alkoxyC₁-C₁₂alkyl,C₁-C₁₂alkylthioC₁-C₁₂alkyl, haloC₁-C₁₂alkylthioC₁-C₁₂alkyl,C₁-C₁₂alkylsulfinyl, haloC₁-C₁₂alkylsulfinyl, C₁-C₁₂alkylsulfonyl,haloC₁-C₁₂alkylsulfonyl, C₁-C₁₂alkylaminosulfonyl,di(C₁-C₁₂alkyl)aminosulfonyl, C₁-C₁₂alkylsulfonylaminocarbonyl,C₁-C₁₂alkylcarbonylaminosulfonyl, C₃-C₁₂cycloalkyloxycarbonyl,C₁-C₁₂alkylcarbonyl, haloC₁-C₁₂alkylcarbonyl, C₁-C₁₂alkoxycarbonyl,haloC₁-C₁₂alkoxycarbonyl, C₁-C₁₂alkylcarbonylC₁-C₁₂alkyl,C₁-C₁₂alkoxycarbonylC₁-C₁₂alkyl, C₁-C₁₂alkylaminocarbonyl,di(C₁-C₁₂alkyl)aminocarbonyl, C₂-C₁₂alkenoxycarbonyl,C₂-C₁₂alkynoxycarbonyl, C₁-C₁₂alkoxyC₁-C₁₂alkoxycarbonyl,C₁-C₁₂alkylaminothio, di(C₁-C₁₂alkyl)aminothio, unsubstituted or furthersubstituted (hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, or (hetero)arylC₁-C₆alkyloxycarbonyl by 1 to 5following groups: halo, NO₂, cyano, C₁-C₆alkyl, haloC₁-C₆alkyl,C₁-C₆alkoxy, or haloC₁-C₆alkoxy; or a salt thereof formed with an acidselected from the group consisting of hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, formic acid, acetic acid, trifluoroaceticacid, oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoicacid, alizaric acid, maleic acid, sorbic acid, malic acid, and citricacid.
 15. The substituted pyrimidine compound according to claim 14,wherein R₁ is C₁-C₈alkyl, C₃-C₈cycloalkyl, C₂-C₈alkenyl,haloC₂-C₈alkenyl, C₂-C₈alkynyl, haloC₂-C₈alkynyl, C₁-C₈alkoxyC₁-C₈alkyl,or haloC₁-C₈alkoxyC₁-C₈alkyl; R₂ is halo, cyano, C₁-C₈alkyl, orhaloC₁-C₈alkoxy; W is H, halo, C₁-C₈alkyl, C₁-C₈alkylthio, orC₁-C₈alkylsulfonyl; R₃ and R₄, may be the same or different, and areeach selected independently from the group consisting of H, C₁-C₈alkyl,C₃-C₈cycloalkyl, C₂-C₈alkenyl, C₂-C₈alkynyl, haloC₂-C₈alkenyl,haloC₂-C₈alkynyl, C₁-C₈alkoxyC₁-C₈alkyl, unsubstituted or furthersubstituted arylC₁-C₄alkyl or heteroarylC₁-C₄alkyl by 1 to 3 followinggroups: halo, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, andhaloC₁-C₄alkoxy; or R₃, R₄ and conjoint carbon can also form a C₃-C₈cycle; R_(5a), R_(5b), and R_(5c), may be the same or different, and areeach selected independently from the group consisting of H,C₃-C₆cycloalkyl, C₁-C₈alkylthio, haloC₁-C₈alkylthio C₃-C₈alkenoxy,haloC₃-C₈alkenoxy, C₃-C₈alkynoxy, haloC₃-C₈alkynoxy, C₁-C₈alkylsulfinyl,haloC₁-C₈alkylsulfinyl, C₁-C₈alkylsulfonyl, haloC₁-C₈alkylsulfonyl,C₁-C₈alkylcarbonyl, haloC₁-C₈alkylcarbonyl, C₁-C₈alkylcarbonyloxy,C₁-C₈alkylcarbonylamino, C₁-C₈alkylsulfonyloxy, C₁-C₈alkoxycarbonyl,C₁-C₈alkoxycarbonylC₁-C₈alkyl, C₁-C₈alkoxycarbonylamino,C₁-C₈alkoxyC₁-C₈alkoxy, and C₁-C₈alkoxycarbonylC₁-C₈alkoxy; X₂ is N orCR₇; X₃ is N or CR₈; X₄ is N or CR₉; X₆ is N or CR₁₁; however, X₂, X₃,X₄, and X₆ are not simultaneously N; R₇, R₈, R₉, and R₁₁, may be thesame or different, and are each selected independently from the groupconsisting of H, halo, OH, cyano, HO(C═O), amino, NO₂, C₁-C₈alkyl,haloC₁-C₈alkyl, C₁-C₈alkoxy, haloC₁-C₈alkoxy, C₁-C₈alkoxycarbonyl,CONH₂, C₁-C₈alkylaminocarbonyl, di(C₁-C₈alkyl)aminocarbonyl,C₁-C₈alkylsulfonyl, and haloC₁-C₈alkylsulfonyl; R₁₀ is H, halo, OH,cyano, HO(C═O), amino, NO₂, C₁-C₈alkyl, haloC₁-C₈alkyl, C₁-C₈alkoxy,haloC₁-C₈alkoxy, C₃-C₈cycloalkyl, C₂-C₈alkenyl, C₂-C₈alkynyl,C₂-C₈alkenoxy, haloC₂-C₈alkenoxy, C₂-C₈alkynoxy, haloC₂-C₈alkynoxy,C₁-C₈alkylthio, haloC₁-C₈alkylthio, C₁-C₈alkoxyC₁-C₈alkyl,haloC₁-C₈alkoxyC₁-C₈alkyl, C₁-C₈alkylthioC₁-C₈alkyl,haloC₁-C₈alkylthioC₁-C₈alkyl, C₁-C₈alkylsulfinyl,haloC₁-C₈alkylsulfinyl, C₁-C₈alkylsulfonyl, haloC₁-C₈alkylsulfonyl,C₁-C₈alkylaminosulfonyl, C₁-C₈alkylamino, haloC₁-C₈alkylamino,di(C₁-C₈alkyl)amino, C₁-C₈alkoxycarbonyl, CONH₂,C₁-C₈alkylaminocarbonyl, di(C₁-C₈alkyl)aminocarbonyl, cyanoC₁-C₈alkoxy,C₁-C₈alkoxycarbonylC₁-C₈alkyl, C₁-C₈alkylaminocarbonylC₁-C₈alkyl, anddi(C₁-C₈alkyl)aminocarbonylC₁-C₈alkyl; A is NR₁₂; B is —CH₂— or—CH₂CH₂—; and R₁₂ is H, OH, H(C)═O, C₁-C₈alkyl, haloC₁-C₈alkyl,C₁-C₈alkoxy, haloC₁-C₈alkoxy, C₃-C₈cycloalkyl, C₁-C₈alkylthio,C₂-C₈alkenylthio, C₂-C₈alkenyl, C₂-C₈alkynyl, haloC₂-C₈alkenyl,haloC₂-C₈alkynyl, C₁-C₈alkoxyC₁-C₈alkyl, haloC₁-C₈alkoxyC₁-C₈alkyl,C₁-C₈alkylthioC₁-C₈alkyl, haloC₁-C₈alkylthioC₁-C₈alkyl,C₁-C₈alkylsulfinyl, haloC₁-C₈alkylsulfinyl, C₁-C₈alkylsulfonyl,haloC₁-C₈alkylsulfonyl, C₁-C₈alkylaminosulfonyl,di(C₁-C₈alkyl)aminosulfonyl, C₁-C₈alkylsulfonylaminocarbonyl,C₁-C₈alkylcarbonylaminosulfonyl, C₃-C₈cycloalkyloxycarbonyl,C₁-C₈alkylcarbonyl, haloC₁-C₈alkylcarbonyl, C₁-C₈alkoxycarbonyl,haloC₁-C₈alkoxycarbonyl, C₁-C₈alkylcarbonylC₁-C₈alkyl,C₁-C₈alkoxycarbonylC₁-C₈alkyl, C₁-C₈alkylaminocarbonyl,di(C₁-C₈alkyl)aminocarbonyl, C₂-C₈alkenoxycarbonyl,C₂-C₈alkynoxycarbonyl, C₁-C₈alkoxyC₁-C₈alkoxycarbonyl,C₁-C₈alkylaminothio, di(C₁-C₈alkyl)aminothio, unsubstituted or furthersubstituted (hetero)arylcarbonylC₁-C₆alkyl, (hetero)arylcarbonyl,(hetero)aryloxycarbonyl, or (hetero)arylC₁-C₆alkyloxycarbonyl by 1 to 3following groups: halo, NO₂, cyano, C₁-C₄alkyl, haloC₁-C₄alkyl,C₁-C₄alkoxy, or haloC₁-C₄alkoxy; or a salt thereof formed with an acidselected from the group consisting of hydrochloric acid, sulfuric acid,nitric acid, phosphoric acid, formic acid, acetic acid, trifluoroaceticacid, oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoicacid, alizaric acid, maleic acid, sorbic acid, malic acid, and citricacid.
 16. The substituted pyrimidine compound according to claim 15,wherein R₁ is C₁-C₄alkyl, C₃-C₆cycloalkyl, C₂-C₄alkenyl,haloC₂-C₄alkenyl, C₂-C₄alkynyl, haloC₂-C₄alkynyl, C₁-C₄alkoxyC₁-C₄alkyl,or haloC₁-C₄alkoxyC₁-C₄alkyl; R₂ is halo or cyano; W is H or CH₃; R₃ andR₄ are H, CH₃, or C₂H₅; R_(5a), R_(5b), and R_(5c), may be the same ordifferent, and are each selected independently from the group consistingof H, C₃-C₆cycloalkyl, C₁-C₄alkylthio, haloC₁-C₄alkylthio,C₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl, C₁-C₄alkylcarbonyl, andC₁-C₄alkoxyC₁-C₄alkoxy; X₂ is N or CR₇; X₃ is N or CR₈; X₄ is N or CR₉;X₆ is N or CR₁₁; however, X₂, X₃, X₄, and X₆ are not simultaneously N;R₇, R₈, R₉, and R₁₁, may be the same or different, and are each selectedindependently from the group consisting of H, halo, OH, cyano, HO(C═O),amino, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₁-C₄alkoxycarbonyl, CONH₂, C₁-C₄alkylaminocarbonyl,di(C₁-C₄alkyl)aminocarbonyl, C₁-C₄alkylsulfonyl, andhaloC₁-C₄alkylsulfonyl; R₁₀ is H, halo, OH, cyano, HO(C═O), amino, NO₂,C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₃-C₄cycloalkyl, C₂-C₄alkenyl, C₂-C₄alkynyl, C₂-C₄alkenoxy,haloC₂-C₄alkenoxy, C₂-C₄alkynoxy, haloC₂-C₄alkynoxy, C₁-C₄alkylthio,haloC₁-C₄alkylthio, C₁-C₄alkoxyC₁-C₄alkyl, haloC₁-C₄alkoxyC₁-C₄alkyl,C₁-C₄alkylthioC₁-C₄alkyl, haloC₁-C₄alkylthioC₁-C₄alkyl,C₁-C₄alkylsulfinyl, haloC₁-C₄alkylsulfinyl, C₁-C₄alkylsulfonyl,haloC₁-C₄alkylsulfonyl, C₁-C₄alkylaminosulfonyl, C₁-C₄alkylamino,haloC₁-C₄alkylamino, di(C₁-C₄alkyl)amino, C₁-C₄alkoxycarbonyl, CONH₂,C₁-C₄alkylaminocarbonyl, di(C₁-C₄alkyl)aminocarbonyl, cyanoC₁-C₁₂alkoxy,C₁-C₄alkoxycarbonylC₁-C₄alkyl, C₁-C₄alkylaminocarbonylC₁-C₄alkyl, ordi(C₁-C₄alkyl)aminocarbonylC₁-C₄alkyl; A is NH; and B is —CH₂— or—CH₂CH₂—; or wherein the salt is formed with hydrochloric acid, sulfuricacid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid,oxalic acid, methylsulfonic acid, p-toluenesulfonic acid, benzoic acid,alizaric acid, maleic acid, sorbic acid, malic acid, or citric acid. 17.The substituted pyrimidine compound according to claim 16, wherein thesubstituted pyrimidine compound is represented by formula III-A, III-B,III-C, III-D, III-E, III-F, III-G, III-H, III-I, or III-J:

wherein R₁ is C₁-C₄alkyl, C₃-C₆cycloalkyl, C₂-C₄alkenyl, C₂-C₄alkynyl,C₁-C₄alkoxyC₁-C₄alkyl, or haloC₁-C₄alkoxyC₁-C₄alkyl; R₂ is halo orcyano; W is H or CH₃; R₃ and R₄ is H, CH₃, or C₂H₅; R_(5a), R_(5b), andR_(5c), may be the same or different, and are each selectedindependently from the group consisting of H and C₁-C₄alkylcarbonyl; R₇,R₈, R₉, and R₁₁, may be the same or different, and are each selectedindependently from the group consisting of H, F, Cl, Br, I, cyano,HO(C═O), NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy,C₁-C₄alkoxycarbonyl, C₁-C₄alkylaminocarbonyl,di(C₁-C₄alkyl)aminocarbonyl, C₁-C₄alkylsulfonyl, andhaloC₁-C₄alkylsulfonyl; R₁₀ is H, F, Cl, Br, I, cyano, NO₂, C₁-C₄alkyl,haloC₁-C₄alkyl, C₁-C₄alkoxy, haloC₁-C₄alkoxy, C₁-C₄alkylsulfonyl, orhaloC₁-C₄alkylsulfonyl; and A is NH; or wherein the salt of formulaIII-A, III-B, III-C, III-D, III-E, III-F, III-G, III-H, III-I, or III-Jis formed with hydrochloric acid, sulfuric acid, phosphoric acid, formicacid, acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonicacid, p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid,sorbic acid, malic acid, or citric acid.
 18. The substituted pyrimidinecompound according to claim 17, wherein the substituted pyrimidinecompound is represented by formula III-A and wherein R₁ is CH₃, or C₂H₅;R₂ is halo or cyano; W is H or CH₃; R₃ and R₄ are H; R_(5a) and R_(5c)are H; R_(5b) is H; R₇, R₈, R₉, and R₁₁, may be the same or different,and are each selected independently from the group consisting of H, F,Cl, Br, cyano, NO₂, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy,haloC₁-C₄alkoxy, C₁-C₄alkoxycarbonyl, C₁-C₄alkylaminocarbonyl,di(C₁-C₄alkyl)aminocarbonyl, C₁-C₄alkylsulfonyl, andhaloC₁-C₄alkylsulfonyl; R₁₀ is H, F, Cl, Br, I, cyano, NO₂,methylsulfonyl, C₁-C₄alkyl, haloC₁-C₄alkyl, C₁-C₄alkoxy, orhaloC₁-C₄alkoxy; and A is NH; or wherein the salt of formula III-A isformed with hydrochloric acid, sulfuric acid, phosphoric acid, formicacid, acetic acid, trifluoroacetic acid, oxalic acid, methylsulfonicacid, p-toluenesulfonic acid, benzoic acid, alizaric acid, maleic acid,sorbic acid, malic acid, or citric acid.
 19. The substituted pyrimidinecompound according to claim 18, wherein R₁ is Cl, CH₃ or C₂H₅; R₂ iscyano; W is H or CH₃; R₃ and R₄ are H; R_(5a) and R_(5c) are H; R_(5b)is H; R₇, R₈, R₉, and R₁₁, may be the same or different, and are eachselected independently from the group consisting of H, F, Cl, CH₃,cyano, NO₂, CF₃, CClF₂, CCl₃, OCH₃, OCF₃, OCH₂CF₃, methylsulfonyl, andtrifluorosulfonyl; R₁₀ is H, F, Cl, CH₃, cyano, NO₂, methylsulfonyl,CF₃, CClF₂, OCH₃, OCF₃, or OCH₂CF₃; and A is NH; or wherein the salt offormula III-A is formed with hydrochloric acid, sulfuric acid,phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalicacid, methylsulfonic acid, p-toluenesulfonic acid, benzoic acid,alizaric acid, maleic acid, sorbic acid, malic acid, or citric acid. 20.A fungicidal, insecticidal, or acaricidal composition comprising one ormore compounds according to claim 1 as an active ingredient, wherein theweight percentage of the active ingredient in the composition is0.1-99%.
 21. A fungicidal, insecticidal, or acaricidal compositioncomprising one or more compounds according to claim 2 as an activeingredient, wherein the weight percentage of the active ingredient inthe composition is 0.1-99%.
 22. A method to control fungus, insects,and/or mites which comprises contacting an effective dose of thecomposition of claim 20 with the fungus, insects, and/or mites, or itsgrowth medium.
 23. A method to control fungus, insects, and/or miteswhich comprises contacting an effective dose of the composition of claim21 with the fungus, insects, and/or mites, or its growth medium.
 24. Afungicidal, insecticidal, or acaricidal composition comprising one ormore compounds according to claim 8 as an active ingredient, wherein theweight percentage of the active ingredient in the composition is0.1-99%.
 25. A method to control fungus, insects, and/or mites whichcomprises contacting an effective dose of the composition of claim 24with the fungus, insects, and/or mites, or its growth medium.
 26. Afungicidal, insecticidal, or acaricidal composition comprising one ormore compounds according to claim 14 as an active ingredient, whereinthe weight percentage of the active ingredient in the composition is0.1-99%.
 27. A method to control fungus, insects, and/or mites whichcomprises contacting an effective dose of the composition of claim 26with the fungus, insects, and/or mites, or its growth medium.